1. Alevy YG, Patel AC, Romero AG, Patel DA, Tucker J, Roswit WT, Miller CA, Heier RF, Byers DE, Brett TJ et al.. (2012) IL-13-induced airway mucus production is attenuated by MAPK13 inhibition.. J Clin Invest, 122 (12): (4555-68). [PMID:23187130] |
2. Adrián FJ, Ding Q, Sim T, Velentza A, Sloan C, Liu Y, Zhang G, Hur W, Ding S, Manley P et al.. (2006) Allosteric inhibitors of Bcr-abl-dependent cell proliferation.. Nat Chem Biol, 2 (2): (95-102). [PMID:16415863] |
3. Greenman C, Stephens P, Smith R, Dalgliesh GL, Hunter C, Bignell G, Davies H, Teague J, Butler A, Stevens C et al.. (2007) Patterns of somatic mutation in human cancer genomes.. Nature, 446 (7132): (153-8). [PMID:17344846] |
4. Lombardo LJ, Lee FY, Chen P, Norris D, Barrish JC, Behnia K, Castaneda S, Cornelius LA, Das J, Doweyko AM et al.. (2004) Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.. J Med Chem, 47 (27): (6658-61). [PMID:15615512] |
5. Mirzoeva S, Sawkar A, Zasadzki M, Guo L, Velentza AV, Dunlap V, Bourguignon JJ, Ramstrom H, Haiech J, Van Eldik LJ et al.. (2002) Discovery of a 3-amino-6-phenyl-pyridazine derivative as a new synthetic antineuroinflammatory compound.. J Med Chem, 31 (45): (563-6). [PMID:11806708] |
6. Szczepankiewicz BG, Kosogof C, Nelson LT, Liu G, Liu B, Zhao H, Serby MD, Xin Z, Liu M, Gum RJ et al.. (2006) Aminopyridine-based c-Jun N-terminal kinase inhibitors with cellular activity and minimal cross-kinase activity.. J Med Chem, 49 (12): (3563-80). [PMID:16759099] |
7. Davis T, Bagley MC, Dix MC, Murziani PG, Rokicki MJ, Widdowson CS, Zayed JM, Bachler MA, Kipling D. (2007) Synthesis and in vivo activity of MK2 and MK2 substrate-selective p38alpha(MAPK) inhibitors in Werner syndrome cells.. Bioorg Med Chem Lett, 17 (24): (6832-5). [PMID:17964780] |
8. Gavrin LK, Green N, Hu Y, Janz K, Kaila N, Li HQ, Tam SY, Thomason JR, Gopalsamy A, Ciszewski G et al.. (2005) Inhibition of Tpl2 kinase and TNF-alpha production with 1,7-naphthyridine-3-carbonitriles: synthesis and structure-activity relationships.. Bioorg Med Chem Lett, 15 (23): (5288-92). [PMID:16165349] |
9. Engler TA, Henry JR, Malhotra S, Cunningham B, Furness K, Brozinick J, Burkholder TP, Clay MP, Clayton J, Diefenbacher C et al.. (2004) Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3.. J Med Chem, 47 (16): (3934-7). [PMID:15267232] |
10. Apsel B, Blair JA, Gonzalez B, Nazif TM, Feldman ME, Aizenstein B, Hoffman R, Williams RL, Shokat KM, Knight ZA. (2008) Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.. Nat Chem Biol, 4 (11): (691-9). [PMID:18849971] |
11. Zarrinkar PP, Gunawardane RN, Cramer MD, Gardner MF, Brigham D, Belli B, Karaman MW, Pratz KW, Pallares G, Chao Q et al.. (2009) AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).. Blood, 114 (14): (2984-92). [PMID:19654408] |
12. Changelian PS, Flanagan ME, Ball DJ, Kent CR, Magnuson KS, Martin WH, Rizzuti BJ, Sawyer PS, Perry BD, Brissette WH et al.. (2003) Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor.. Science, 302 (5646): (875-8). [PMID:14593182] |
13. Conway JG, McDonald B, Parham J, Keith B, Rusnak DW, Shaw E, Jansen M, Lin P, Payne A, Crosby RM et al.. (2005) Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.. Proc Natl Acad Sci USA, 102 (44): (16078-83). [PMID:16249345] |
14. Goodfellow VS, Loweth CJ, Ravula SB, Wiemann T, Nguyen T, Xu Y, Todd DE, Sheppard D, Pollack S, Polesskaya O et al.. (2013) Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.. J Med Chem, 56 (20): (8032-48). [PMID:24044867] |
15. Lafleur K, Huang D, Zhou T, Caflisch A, Nevado C. (2009) Structure-based optimization of potent and selective inhibitors of the tyrosine kinase erythropoietin producing human hepatocellular carcinoma receptor B4 (EphB4).. J Med Chem, 52 (20): (6433-46). [PMID:19788238] |
16. Pandey A, Volkots DL, Seroogy JM, Rose JW, Yu JC, Lambing JL, Hutchaleelaha A, Hollenbach SJ, Abe K, Giese NA et al.. (2002) Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family.. J Med Chem, 45 (17): (3772-93). [PMID:12166950] |
17. Millan DS, Bunnage ME, Burrows JL, Butcher KJ, Dodd PG, Evans TJ, Fairman DA, Hughes SJ, Kilty IC, Lemaitre A et al.. (2011) Design and synthesis of inhaled p38 inhibitors for the treatment of chronic obstructive pulmonary disease.. J Med Chem, 54 (22): (7797-814). [PMID:21888439] |
18. Okuzumi T, Fiedler D, Zhang C, Gray DC, Aizenstein B, Hoffman R, Shokat KM. (2009) Inhibitor hijacking of Akt activation.. Nat Chem Biol, 5 (7): (484-93). [PMID:19465931] |
19. Milkiewicz KL, Aimone LD, Albom MS, Angeles TS, Chang H, Grobelny JV, Husten J, Losardo C, Miknyoczki S, Murthy S et al.. (2011) Improvement in oral bioavailability of 2,4-diaminopyrimidine c-Met inhibitors by incorporation of a 3-amidobenzazepin-2-one group.. Bioorg Med Chem, 19 (21): (6274-84). [PMID:21967808] |
20. Li B, Cociorva OM, Nomanbhoy T, Weissig H, Li Q, Nakamura K, Liyanage M, Zhang MC, Shih AY, Aban A et al.. (2013) Hit-to-lead optimization and kinase selectivity of imidazo[1,2-a]quinoxalin-4-amine derived JNK1 inhibitors.. Bioorg Med Chem Lett, 23 (18): (5217-22). [PMID:23916259] |
21. Miwatashi S, Arikawa Y, Kotani E, Miyamoto M, Naruo K, Kimura H, Tanaka T, Asahi S, Ohkawa S. (2005) Novel inhibitor of p38 MAP kinase as an anti-TNF-alpha drug: discovery of N-[4-[2-ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl]-2-pyridyl]benzamide (TAK-715) as a potent and orally active anti-rheumatoid arthritis agent.. J Med Chem, 48 (19): (5966-79). [PMID:16162000] |
22. Aronov AM, Tang Q, Martinez-Botella G, Bemis GW, Cao J, Chen G, Ewing NP, Ford PJ, Germann UA, Green J et al.. (2009) Structure-guided design of potent and selective pyrimidylpyrrole inhibitors of extracellular signal-regulated kinase (ERK) using conformational control.. J Med Chem, 52 (20): (6362-8). [PMID:19827834] |
23. Hobson AD, Harris CM, van der Kam EL, Turner SC, Abibi A, Aguirre AL, Bousquet P, Kebede T, Konopacki DB, Gintant G et al.. (2015) Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.. J Med Chem, 58 (23): (9154-70). [PMID:26509640] |
24. Albrecht W, Unger A, Bauer SM, Laufer SA. (2017) Discovery of N-{4-[5-(4-Fluorophenyl)-3-methyl-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-acetamide (CBS-3595), a Dual p38α MAPK/PDE-4 Inhibitor with Activity against TNFα-Related Diseases.. J Med Chem, 60 (13): (5290-5305). [PMID:28613871] |
25. He X, Da Ros S, Nelson J, Zhu X, Jiang T, Okram B, Jiang S, Michellys PY, Iskandar M, Espinola S et al.. (2017) Identification of Potent and Selective RIPK2 Inhibitors for the Treatment of Inflammatory Diseases.. ACS Med Chem Lett, 8 (10): (1048-1053). [PMID:29057049] |
26. Tan L, Gurbani D, Weisberg EL, Jones DS, Rao S, Singer WD, Bernard FM, Mowafy S, Jenney A, Du G et al.. (2017) Studies of TAK1-centered polypharmacology with novel covalent TAK1 inhibitors.. Bioorg Med Chem, 25 (4): (1320-1328). [PMID:28038940] |
27. Laleu B, Gaggini F, Orchard M, Fioraso-Cartier L, Cagnon L, Houngninou-Molango S, Gradia A, Duboux G, Merlot C, Heitz F et al.. (2010) First in class, potent, and orally bioavailable NADPH oxidase isoform 4 (Nox4) inhibitors for the treatment of idiopathic pulmonary fibrosis.. J Med Chem, 53 (21): (7715-30). [PMID:20942471] |
28. Li Y, Xiong Y, Zhang G, Zhang L, Yang W, Yang J, Huang L, Qiao Z, Miao Z, Lin G et al.. (2018) Identification of 5-(2,3-Dihydro-1 H-indol-5-yl)-7 H-pyrrolo[2,3- d]pyrimidin-4-amine Derivatives as a New Class of Receptor-Interacting Protein Kinase 1 (RIPK1) Inhibitors, Which Showed Potent Activity in a Tumor Metastasis Model.. J Med Chem, 61 (24): (11398-11414). [PMID:30480444] |
29. Pomel V, Klicic J, Covini D, Church DD, Shaw JP, Roulin K, Burgat-Charvillon F, Valognes D, Camps M, Chabert C et al.. (2006) Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase gamma.. J Med Chem, 49 (13): (3857-71). [PMID:16789742] |
30. Erik Rytter Ottosen,Morten Dahl Sørensen,Fredrik Björkling,Tine Skak-Nielsen,Marianne Scheel Fjording,Helle Aaes,Lise Binderup. (2003-12-12) Synthesis and structure-activity relationship of aminobenzophenones. A novel class of p38 MAP kinase inhibitors with high antiinflammatory activity.. Journal of medicinal chemistry, 46 ((26)): (5651-5662). [PMID:14667219] |
31. Erki Enkvist, Darja Lavogina, Gerda Raidaru, Angela Vaasa, Indrek Viil, Marje Lust, Kaido Viht, Asko Uri,. (2006-11-28) Conjugation of adenosine and hexa-(D-arginine) leads to a nanomolar bisubstrate-analog inhibitor of basophilic protein kinases.. Journal of medicinal chemistry, 49 ((24)): ( 7150-7159 ). [PMID:17125267] |
32. Henry JR, Rupert KC, Dodd JH, Turchi IJ, Wadsworth SA, Cavender DE, Schafer PH, Siekierka JJ.. (1998) Potent inhibitors of the MAP kinase p38.. Bioorg Med Chem Lett, 8 (23): (3335-3340). [PMID:9873730] |
33. Revesz L, Di Padova FE, Buhl T, Feifel R, Gram H, Hiestand P, Manning U, Zimmerlin AG.. (2000) SAR of 4-hydroxypiperidine and hydroxyalkyl substituted heterocycles as novel p38 map kinase inhibitors.. Bioorg Med Chem Lett, 10 (11): (1261-1264). [PMID:10866395] |
34. Rupert KC, Henry JR, Dodd JH, Wadsworth SA, Cavender DE, Olini GC, Fahmy B, Siekierka JJ.. (2003) Imidazopyrimidines, potent inhibitors of p38 MAP kinase.. Bioorg Med Chem Lett, 13 (3): (347-350). [PMID:12565927] |
35. Boehm JC, Smietana JM, Sorenson ME, Garigipati RS, Gallagher TF, Sheldrake PL, Bradbeer J, Badger AM, Laydon JT, Lee JC, Hillegass LM, Griswold DE, Breton JJ, Chabot-Fletcher MC, Adams JL.. (1996) 1-substituted 4-aryl-5-pyridinylimidazoles: a new class of cytokine suppressive drugs with low 5-lipoxygenase and cyclooxygenase inhibitory potency.. J Med Chem, 39 (20): (3929-3937). [PMID:8831759] |
36. Liverton NJ, Butcher JW, Claiborne CF, Claremon DA, Libby BE, Nguyen KT, Pitzenberger SM, Selnick HG, Smith GR, Tebben A, Vacca JP, Varga SL, Agarwal L, Dancheck K, Forsyth AJ, Fletcher DS, Frantz B, Hanlon WA, Harper CF, Hofsess SJ, Kostura M, Lin J, Luell S, O'Neill EA, O'Keefe SJ.. (1999) Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase.. J Med Chem, 42 (12): (2180-2190). [PMID:10377223] |
37. McKenna JM, Halley F, Souness JE, McLay IM, Pickett SD, Collis AJ, Page K, Ahmed I.. (2002) An algorithm-directed two-component library synthesized via solid-phase methodology yielding potent and orally bioavailable p38 MAP kinase inhibitors.. J Med Chem, 45 (11): (2173-2184). [PMID:12014955] |
38. Trejo A, Arzeno H, Browner M, Chanda S, Cheng S, Comer DD, Dalrymple SA, Dunten P, Lafargue J, Lovejoy B, Freire-Moar J, Lim J, Mcintosh J, Miller J, Papp E, Reuter D, Roberts R, Sanpablo F, Saunders J, Song K, Villasenor A, Warren SD, Welch M, Weller P, Whiteley PE, Zeng L, Goldstein DM.. (2003) Design and synthesis of 4-azaindoles as inhibitors of p38 MAP kinase.. J Med Chem, 46 (22): (4702-4713). [PMID:14561090] |
39. Gellibert F, Woolven J, Fouchet MH, Mathews N, Goodland H, Lovegrove V, Laroze A, Nguyen VL, Sautet S, Wang R, Janson C, Smith W, Krysa G, Boullay V, De Gouville AC, Huet S, Hartley D.. (2004) Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors.. J Med Chem, 47 (18): (4494-4506). [PMID:15317461] |
40. VanderWel SN, Harvey PJ, McNamara DJ, Repine JT, Keller PR, Quin J, Booth RJ, Elliott WL, Dobrusin EM, Fry DW, Toogood PL.. (2005) Pyrido[2,3-d]pyrimidin-7-ones as specific inhibitors of cyclin-dependent kinase 4.. J Med Chem, 48 (7): (2371-2387). [PMID:15801830] |
41. Zhao H, Serby MD, Xin Z, Szczepankiewicz BG, Liu M, Kosogof C, Liu B, Nelson LT, Johnson EF, Wang S, Pederson T, Gum RJ, Clampit JE, Haasch DL, Abad-Zapatero C, Fry EH, Rondinone C, Trevillyan JM, Sham HL, Liu G.. (2006) Discovery of potent, highly selective, and orally bioavailable pyridine carboxamide c-Jun NH2-terminal kinase inhibitors.. J Med Chem, 49 (15): (4455-4458). [PMID:16854050] |
42. Borzilleri RM, Bhide RS, Barrish JC, D'Arienzo CJ, Derbin GM, Fargnoli J, Hunt JT, Jeyaseelan R, Kamath A, Kukral DW, Marathe P, Mortillo S, Qian L, Tokarski JS, Wautlet BS, Zheng X, Lombardo LJ.. (2006) Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2.. J Med Chem, 49 (13): (3766-3769). [PMID:16789733] |
43. Natarajan SR, Liu L, Levorse M, Thompson JE, O'Neill EA, O'Keefe SJ, Vora KA, Cvetovich R, Chung JY, Carballo-Jane E, Visco DM.. (2006) p38 MAP kinase inhibitors. Part 5: discovery of an orally bio-available and highly efficacious compound based on the 7-amino-naphthyridone scaffold.. Bioorg Med Chem Lett, 16 (20): (5468-5471). [PMID:16945534] |
44. Hu Y, Green N, Gavrin LK, Janz K, Kaila N, Li HQ, Thomason JR, Cuozzo JW, Hall JP, Hsu S, Nickerson-Nutter C, Telliez JB, Lin LL, Tam S.. (2006) Inhibition of Tpl2 kinase and TNFalpha production with quinoline-3-carbonitriles for the treatment of rheumatoid arthritis.. Bioorg Med Chem Lett, 16 (23): (6067-6072). [PMID:16973359] |
45. Bruno O, Brullo C, Bondavalli F, Schenone S, Ranise A, Arduino N, Bertolotto MB, Montecucco F, Ottonello L, Dallegri F, Tognolini M, Ballabeni V, Bertoni S, Barocelli E.. (2007) Synthesis and biological evaluation of N-pyrazolyl-N'-alkyl/benzyl/phenylureas: a new class of potent inhibitors of interleukin 8-induced neutrophil chemotaxis.. J Med Chem, 50 (15): (3618-3626). [PMID:17608466] |
46. Cincinelli R, Dallavalle S, Nannei R, Merlini L, Penco S, Giannini G, Pisano C, Vesci L, Ferrara FF, Zuco V, Zanchi C, Zunino F.. (2007) Synthesis and structure-activity relationships of new antiproliferative and proapoptotic retinoid-related biphenyl-4-yl-acrylic acids.. Bioorg Med Chem, 15 (14): (4863-4875). [PMID:17512204] |
47. Singh RK, Lange TS, Kim K, Zou Y, Lieb C, Sholler GL, Brard L.. (2007) Effect of indole ethyl isothiocyanates on proliferation, apoptosis, and MAPK signaling in neuroblastoma cell lines.. Bioorg Med Chem Lett, 17 (21): (5846-5852). [PMID:17855093] |
48. Graneto MJ, Kurumbail RG, Vazquez ML, Shieh HS, Pawlitz JL, Williams JM, Stallings WC, Geng L, Naraian AS, Koszyk FJ, Stealey MA, Xu XD, Weier RM, Hanson GJ, Mourey RJ, Compton RP, Mnich SJ, Anderson GD, Monahan JB, Devraj R.. (2007) Synthesis, crystal structure, and activity of pyrazole-based inhibitors of p38 kinase.. J Med Chem, 50 (23): (5712-5719). [PMID:17948975] |
49. Varma H, Cheng R, Voisine C, Hart AC, Stockwell BR.. (2007) Inhibitors of metabolism rescue cell death in Huntington's disease models.. Proc Natl Acad Sci U S A, 104 (36): (14525-14530). [PMID:17726098] |
50. Feng R, Ni HM, Wang SY, Tourkova IL, Shurin MR, Harada H, Yin XM.. (2007) Cyanidin-3-rutinoside, a natural polyphenol antioxidant, selectively kills leukemic cells by induction of oxidative stress.. J Biol Chem, 282 (18): (13468-13476). [PMID:17360708] |
51. Feng Y, Yin Y, Weiser A, Griffin E, Cameron MD, Lin L, Ruiz C, Schürer SC, Inoue T, Rao PV, Schröter T, Lograsso P.. (2008) Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors.. J Med Chem, 51 (21): (6642-6645). [PMID:18834107] |
52. Lumeras W, Caturla F, Vidal L, Esteve C, Balagué C, Orellana A, Domínguez M, Roca R, Huerta JM, Godessart N, Vidal B.. (2009) Design, synthesis, and structure-activity relationships of aminopyridine N-oxides, a novel scaffold for the potent and selective inhibition of p38 mitogen activated protein kinase.. J Med Chem, 52 (17): (5531-5545). [PMID:19678708] |
53. Li Q, Al-Ayoubi A, Guo T, Zheng H, Sarkar A, Nguyen T, Eblen ST, Grant S, Kellogg GE, Zhang S.. (2009) Structure-activity relationship (SAR) studies of 3-(2-amino-ethyl)-5-(4-ethoxy-benzylidene)-thiazolidine-2,4-dione: development of potential substrate-specific ERK1/2 inhibitors.. Bioorg Med Chem Lett, 19 (21): (6042-6046). [PMID:19796943] |
54. Li J, Kaoud TS, Laroche C, Dalby KN, Kerwin SM.. (2009) Synthesis and biological evaluation of p38alpha kinase-targeting dialkynylimidazoles.. Bioorg Med Chem Lett, 19 (22): (6293-6297). [PMID:19822424] |
55. Qiao L, Choi S, Case A, Gainer TG, Seyb K, Glicksman MA, Lo DC, Stein RL, Cuny GD.. (2009) Structure-activity relationship study of EphB3 receptor tyrosine kinase inhibitors.. Bioorg Med Chem Lett, 19 (21): (6122-6126). [PMID:19783434] |
56. Pettus LH, Wurz RP, Xu S, Herberich B, Henkle B, Liu Q, McBride HJ, Mu S, Plant MH, Saris CJ, Sherman L, Wong LM, Chmait S, Lee MR, Mohr C, Hsieh F, Tasker AS.. (2010) Discovery and evaluation of 7-alkyl-1,5-bis-aryl-pyrazolopyridinones as highly potent, selective, and orally efficacious inhibitors of p38alpha mitogen-activated protein kinase.. J Med Chem, 53 (7): (2973-2985). [PMID:20218619] |
57. Deng X, Lim SM, Zhang J, Gray NS.. (2010) Broad spectrum alkynyl inhibitors of T315I Bcr-Abl.. Bioorg Med Chem Lett, 20 (14): (4196-4200). [PMID:20541934] |
58. Nakao A, Ohkawa N, Nagasaki T, Kagari T, Doi H, Shimozato T, Ushiyama S, Aoki K.. (2010) Tetrahydropyridine derivatives with inhibitory activity on the production of proinflammatory cytokines: part 3.. Bioorg Med Chem Lett, 20 (16): (4774-4778). [PMID:20637613] |
59. Terazawa R, Garud DR, Hamada N, Fujita Y, Itoh T, Nozawa Y, Nakane K, Deguchi T, Koketsu M, Ito M.. (2010) Identification of organoselenium compounds that possess chemopreventive properties in human prostate cancer LNCaP cells.. Bioorg Med Chem, 18 (19): (7001-7008). [PMID:20805033] |
60. Probst GD, Bowers S, Sealy JM, Truong AP, Hom RK, Galemmo RA, Konradi AW, Sham HL, Quincy DA, Pan H, Yao N, Lin M, Tóth G, Artis DR, Zmolek W, Wong K, Qin A, Lorentzen C, Nakamura DF, Quinn KP, Sauer JM, Powell K, Ruslim L, Wright S, Chereau D, Ren Z, Anderson JP, Bard F, Yednock TA, Griswold-Prenner I.. (2011) Highly selective c-Jun N-terminal kinase (JNK) 2 and 3 inhibitors with in vitro CNS-like pharmacokinetic properties prevent neurodegeneration.. Bioorg Med Chem Lett, 21 (1): (315-319). [PMID:21112785] |
61. Mandal PK, Gao F, Lu Z, Ren Z, Ramesh R, Birtwistle JS, Kaluarachchi KK, Chen X, Bast RC, Liao WS, McMurray JS.. (2011) Potent and selective phosphopeptide mimetic prodrugs targeted to the Src homology 2 (SH2) domain of signal transducer and activator of transcription 3.. J Med Chem, 54 (10): (3549-3563). [PMID:21486047] |
62. Lumeras W, Vidal L, Vidal B, Balagué C, Orellana A, Maldonado M, Domínguez M, Segarra V, Caturla F.. (2011) 1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.. J Med Chem, 54 (22): (7899-7910). [PMID:21999461] |
63. Festa M, Capasso A, D'Acunto CW, Masullo M, Rossi AG, Pizza C, Piacente S.. (2011) Xanthohumol induces apoptosis in human malignant glioblastoma cells by increasing reactive oxygen species and activating MAPK pathways.. J Nat Prod, 74 (12): (2505-2513). [PMID:22111577] |
64. Yang T, Lu Z, Meng L, Wei S, Hong K, Zhu W, Huang C.. (2012) The novel agent ophiobolin O induces apoptosis and cell cycle arrest of MCF-7 cells through activation of MAPK signaling pathways.. Bioorg Med Chem Lett, 22 (1): (579-585). [PMID:22130129] |
65. Cuny GD, Ulyanova NP, Patnaik D, Liu JF, Lin X, Auerbach K, Ray SS, Xian J, Glicksman MA, Stein RL, Higgins JM.. (2012) Structure-activity relationship study of beta-carboline derivatives as haspin kinase inhibitors.. Bioorg Med Chem Lett, 22 (5): (2015-2019). [PMID:22335895] |
66. Zhang J, Deng X, Choi HG, Alessi DR, Gray NS.. (2012) Characterization of TAE684 as a potent LRRK2 kinase inhibitor.. Bioorg Med Chem Lett, 22 (5): (1864-1869). [PMID:22335897] |
67. Maryanoff BE, O'Neill JC, McComsey DF, Yabut SC, Luci DK, Jordan AD, Masucci JA, Jones WJ, Abad MC, Gibbs AC, Petrounia I.. (2011) Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site.. ACS Med Chem Lett, 2 (7): (538-543). [PMID:24900346] |
68. Andreani A, Granaiola M, Locatelli A, Morigi R, Rambaldi M, Varoli L, Calonghi N, Cappadone C, Farruggia G, Stefanelli C, Masotti L, Nguyen TL, Hamel E, Shoemaker RH.. (2012) Substituted 3-(5-imidazo[2,1-b]thiazolylmethylene)-2-indolinones and analogues: synthesis, cytotoxic activity, and study of the mechanism of action.. J Med Chem, 55 (5): (2078-2088). [PMID:22283430] |
69. Maryanoff BE, O'Neill JC, McComsey DF, Yabut SC, Luci DK, Gibbs AC, Connelly MA.. (2012) Pyrimidinopyrimidine inhibitors of ketohexokinase: exploring the ring C2 group that interacts with Asp-27B in the ligand binding pocket.. Bioorg Med Chem Lett, 22 (16): (5326-5329). [PMID:22795331] |
70. Kwon OW, Moon E, Chari MA, Kim TW, Kim AJ, Lee P, Ahn KH, Kim SY.. (2012) A substituted 3,4-dihydropyrimidinone derivative (compound D22) prevents inflammation mediated neurotoxicity; role in microglial activation in BV-2 cells.. Bioorg Med Chem Lett, 22 (16): (5199-5203). [PMID:22819763] |
71. Malmström J, Viklund J, Slivo C, Costa A, Maudet M, Sandelin C, Hiller G, Olsson LL, Aagaard A, Geschwindner S, Xue Y, Vasänge M.. (2012) Synthesis and structure-activity relationship of 4-(1,3-benzothiazol-2-yl)-thiophene-2-sulfonamides as cyclin-dependent kinase 5 (cdk5)/p25 inhibitors.. Bioorg Med Chem Lett, 22 (18): (5919-5923). [PMID:22889803] |
72. Srivatsan A, Wang Y, Joshi P, Sajjad M, Chen Y, Liu C, Thankppan K, Missert JR, Tracy E, Morgan J, Rigual N, Baumann H, Pandey RK.. (2011) In vitro cellular uptake and dimerization of signal transducer and activator of transcription-3 (STAT3) identify the photosensitizing and imaging-potential of isomeric photosensitizers derived from chlorophyll-a and bacteriochlorophyll-a.. J Med Chem, 54 (19): (6859-6873). [PMID:21842893] |
73. Illig CR, Manthey CL, Wall MJ, Meegalla SK, Chen J, Wilson KJ, Ballentine SK, Desjarlais RL, Schubert C, Crysler CS, Chen Y, Molloy CJ, Chaikin MA, Donatelli RR, Yurkow E, Zhou Z, Player MR, Tomczuk BE.. (2011) Optimization of a potent class of arylamide colony-stimulating factor-1 receptor inhibitors leading to anti-inflammatory clinical candidate 4-cyano-N-[2-(1-cyclohexen-1-yl)-4-[1-[(dimethylamino)acetyl]-4-piperidinyl]phenyl]-1H-imidazole-2-carboxamide (JNJ-28312141).. J Med Chem, 54 (22): (7860-7883). [PMID:22039836] |
74. Park EJ, Kiselev E, Conda-Sheridan M, Cushman M, Pezzuto JM.. (2012) Induction of apoptosis by 3-amino-6-(3-aminopropyl)-5,6-dihydro-5,11-dioxo-11H-indeno[1,2-c]isoquinoline via modulation of MAPKs (p38 and c-Jun N-terminal kinase) and c-Myc in HL-60 human leukemia cells.. J Nat Prod, 75 (3): (378-384). [PMID:22148260] |
75. Asano T, Yamazaki H, Kasahara C, Kubota H, Kontani T, Harayama Y, Ohno K, Mizuhara H, Yokomoto M, Misumi K, Kinoshita T, Ohta M, Takeuchi M.. (2012) Identification, synthesis, and biological evaluation of 6-[(6R)-2-(4-fluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3(2H)-one (AS1940477), a potent p38 MAP kinase inhibitor.. J Med Chem, 55 (17): (7772-7785). [PMID:22905713] |
76. Huh JE, Kang JW, Nam D, Baek YH, Choi DY, Park DS, Lee JD.. (2012) Melittin suppresses VEGF-A-induced tumor growth by blocking VEGFR-2 and the COX-2-mediated MAPK signaling pathway.. J Nat Prod, 75 (11): (1922-1929). [PMID:23110475] |
77. Reith AD, Bamborough P, Jandu K, Andreotti D, Mensah L, Dossang P, Choi HG, Deng X, Zhang J, Alessi DR, Gray NS.. (2012) GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor.. Bioorg Med Chem Lett, 22 (17): (5625-5629). [PMID:22863203] |
78. Gong L, Tan YC, Boice G, Abbot S, McCaleb K, Iyer P, Zuo F, Dal Porto J, Wong B, Jin S, Chang A, Tran P, Hsieh G, Niu L, Shao A, Reuter D, Lukacs CM, Ursula Kammlott R, Kuglstatter A, Goldstein D.. (2012) Discovery of a novel series of 4-quinolone JNK inhibitors.. Bioorg Med Chem Lett, 22 (24): (7381-7387). [PMID:23142618] |
79. Dolečková I, Cesnek M, Dračinský M, Brynda J, Voller J, Janeba Z, Kryštof V.. (2013) Synthesis and biological evaluation of guanidino analogues of roscovitine.. Eur J Med Chem, 62 (443-452). [PMID:23399722] |
80. Yin Y, Lin L, Ruiz C, Khan S, Cameron MD, Grant W, Pocas J, Eid N, Park H, Schröter T, Lograsso PV, Feng Y.. (2013) Synthesis and biological evaluation of urea derivatives as highly potent and selective rho kinase inhibitors.. J Med Chem, 56 (9): (3568-3581). [PMID:23570561] |
81. Mortensen DS, Sapienza J, Lee BG, Perrin-Ninkovic SM, Harris R, Shevlin G, Parnes JS, Whitefield B, Hickman M, Khambatta G, Bisonette RR, Peng S, Gamez JC, Leisten J, Narla RK, Fultz KE, Sankar S.. (2013) Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.. Bioorg Med Chem Lett, 23 (6): (1588-1591). [PMID:23414803] |
82. Olajide OA, Bhatia HS, de Oliveira AC, Wright CW, Fiebich BL.. (2013) Anti-neuroinflammatory properties of synthetic cryptolepine in human neuroblastoma cells: possible involvement of NF-κB and p38 MAPK inhibition.. Eur J Med Chem, 63 (333-339). [PMID:23507189] |
83. Jiang R, Frackowiak B, Shin Y, Song X, Chen W, Lin L, Cameron MD, Duckett DR, Kamenecka TM.. (2013) Design and synthesis of 1-aryl-5-anilinoindazoles as c-Jun N-terminal kinase inhibitors.. Bioorg Med Chem Lett, 23 (9): (2683-2687). [PMID:23518277] |
84. Wright LE, Frye JB, Lukefahr AL, Timmermann BN, Mohammad KS, Guise TA, Funk JL.. (2013) Curcuminoids block TGF-β signaling in human breast cancer cells and limit osteolysis in a murine model of breast cancer bone metastasis.. J Nat Prod, 76 (3): (316-321). [PMID:23145932] |
85. Bowers S, Truong AP, Ye M, Aubele DL, Sealy JM, Neitz RJ, Hom RK, Chan W, Dappen MS, Galemmo RA, Konradi AW, Sham HL, Zhu YL, Beroza P, Tonn G, Zhang H, Hoffman J, Motter R, Fauss D, Tanaka P, Bova MP, Ren Z, Tam D, Ruslim L, Baker J, Pandya D, Diep L, Fitzgerald K, Artis DR, Anderson JP, Bergeron M.. (2013) Design and synthesis of highly selective, orally active Polo-like kinase-2 (Plk-2) inhibitors.. Bioorg Med Chem Lett, 23 (9): (2743-2749). [PMID:23522834] |
86. Akama T, Dong C, Virtucio C, Freund YR, Chen D, Orr MD, Jacobs RT, Zhang YK, Hernandez V, Liu Y, Wu A, Bu W, Liu L, Jarnagin K, Plattner JJ.. (2013) Discovery and structure-activity relationships of 6-(benzoylamino)benzoxaboroles as orally active anti-inflammatory agents.. Bioorg Med Chem Lett, 23 (21): (5870-5873). [PMID:24075731] |
87. Hanke T, Dehm F, Liening S, Popella SD, Maczewsky J, Pillong M, Kunze J, Weinigel C, Barz D, Kaiser A, Wurglics M, Lämmerhofer M, Schneider G, Sautebin L, Schubert-Zsilavecz M, Werz O.. (2013) Aminothiazole-featured pirinixic acid derivatives as dual 5-lipoxygenase and microsomal prostaglandin E2 synthase-1 inhibitors with improved potency and efficiency in vivo.. J Med Chem, 56 (22): (9031-9044). [PMID:24171493] |
88. He Y, Duckett D, Chen W, Ling YY, Cameron MD, Lin L, Ruiz CH, Lograsso PV, Kamenecka TM, Koenig M.. (2014) Synthesis and SAR of novel isoxazoles as potent c-jun N-terminal kinase (JNK) inhibitors.. Bioorg Med Chem Lett, 24 (1): (161-164). [PMID:24332487] |
89. Maciag AE, Holland RJ, Kim Y, Kumari V, Luthers CE, Sehareen WS, Biswas D, Morris NL, Ji X, Anderson LM, Saavedra JE, Keefer LK.. (2014) Nitric oxide (NO) releasing poly ADP-ribose polymerase 1 (PARP-1) inhibitors targeted to glutathione S-transferase P1-overexpressing cancer cells.. J Med Chem, 57 (6): (2292-2302). [PMID:24521039] |
90. Park CH, Lee C, Yang JS, Joe BY, Chun K, Kim H, Kim HY, Kang JS, Lee JI, Kim MH, Han G.. (2014) Discovery of thienopyrimidine-based FLT3 inhibitors from the structural modification of known IKKβ inhibitors.. Bioorg Med Chem Lett, 24 (12): (2655-2660). [PMID:24813730] |
91. Cho N, Yang H, Kim JW, Kim YC, Sung SH.. (2014) Chemical constituents isolated from Disporum viridescens leaves and their inhibitory effect on nitric oxide production in BV2 microglial cells.. Bioorg Med Chem Lett, 24 (24): (5675-5678). [PMID:25467159] |
92. Tseng CH, Tzeng CC, Chiu CC, Hsu CY, Chou CK, Chen YL.. (2015) Discovery of 2-[2-(5-nitrofuran-2-yl)vinyl]quinoline derivatives as a novel type of antimetastatic agents.. Bioorg Med Chem, 23 (1): (141-148). [PMID:25467291] |
93. Hasumi K, Sato S, Saito T, Kato JY, Shirota K, Sato J, Suzuki H, Ohta S.. (2014) Design and synthesis of 5-[(2-chloro-6-fluorophenyl)acetylamino]-3-(4-fluorophenyl)-4-(4-pyrimidinyl)isoxazole (AKP-001), a novel inhibitor of p38 MAP kinase with reduced side effects based on the antedrug concept.. Bioorg Med Chem, 22 (15): (4162-4176). [PMID:24938496] |
94. Carry JC, Clerc F, Minoux H, Schio L, Mauger J, Nair A, Parmantier E, Le Moigne R, Delorme C, Nicolas JP, Krick A, Abécassis PY, Crocq-Stuerga V, Pouzieux S, Delarbre L, Maignan S, Bertrand T, Bjergarde K, Ma N, Lachaud S, Guizani H, Lebel R, Doerflinger G, Monget S, Perron S, Gasse F, Angouillant-Boniface O, Filoche-Rommé B, Murer M, Gontier S, Prévost C, Monteiro ML, Combeau C.. (2015) SAR156497, an exquisitely selective inhibitor of aurora kinases.. J Med Chem, 58 (1): (362-375). [PMID:25369539] |
95. Koch P, Gehringer M, Laufer SA.. (2015) Inhibitors of c-Jun N-terminal kinases: an update.. J Med Chem, 58 (1): (72-95). [PMID:25415535] |
96. Chen WY, Chen FY, Lee AS, Ting KH, Chang CM, Hsu JF, Lee WS, Sheu JR, Chen CH, Shen MY.. (2015) Sesamol reduces the atherogenicity of electronegative L5 LDL in vivo and in vitro.. J Nat Prod, 78 (2): (225-233). [PMID:25692815] |
97. Henry JR, Kaufman MD, Peng SB, Ahn YM, Caldwell TM, Vogeti L, Telikepalli H, Lu WP, Hood MM, Rutkoski TJ, Smith BD, Vogeti S, Miller D, Wise SC, Chun L, Zhang X, Zhang Y, Kays L, Hipskind PA, Wrobleski AD, Lobb KL, Clay JM, Cohen JD, Walgren JL, McCann D, Patel P, Clawson DK, Guo S, Manglicmot D, Groshong C, Logan C, Starling JJ, Flynn DL.. (2015) Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells.. J Med Chem, 58 (10): (4165-4179). [PMID:25965804] |
98. Zhou X, Wang Y, Lee WY, Or PM, Wan DC, Kwan YW, Yeung JH.. (2015) Miltirone Is a Dual Inhibitor of P-Glycoprotein and Cell Growth in Doxorubicin-Resistant HepG2 Cells.. J Nat Prod, 78 (9): (2266-2275). [PMID:26339922] |
99. Charnley AK, Convery MA, Lakdawala Shah A, Jones E, Hardwicke P, Bridges A, Ouellette M, Totoritis R, Schwartz B, King BW, Wisnoski DD, Kang J, Eidam PM, Votta BJ, Gough PJ, Marquis RW, Bertin J, Casillas L.. (2015) Crystal structures of human RIP2 kinase catalytic domain complexed with ATP-competitive inhibitors: Foundations for understanding inhibitor selectivity.. Bioorg Med Chem, 23 (21): (7000-7006). [PMID:26455654] |
100. Lee NY, Chung KS, Jin JS, Bang KS, Eom YJ, Hong CH, Nugroho A, Park HJ, An HJ.. (2015) Effect of Chicoric Acid on Mast Cell-Mediated Allergic Inflammation in Vitro and in Vivo.. J Nat Prod, 78 (12): (2956-2962). [PMID:26593037] |
101. Schiemann K, Mallinger A, Wienke D, Esdar C, Poeschke O, Busch M, Rohdich F, Eccles SA, Schneider R, Raynaud FI, Czodrowski P, Musil D, Schwarz D, Urbahns K, Blagg J.. (2016) Discovery of potent and selective CDK8 inhibitors from an HSP90 pharmacophore.. Bioorg Med Chem Lett, 26 (5): (1443-1451). [PMID:26852363] |
102. Juszczak M, Walczak K, Matysiak J, Lemieszek MK, Langner E, Karpińska MM, Pożarowski P, Niewiadomy A, Rzeski W.. (2016) New derivative of 2-(2,4-dihydroxyphenyl)thieno-1,3-thiazin-4-one (BChTT) elicits antiproliferative effect via p38-mediated cell cycle arrest in cancer cells.. Bioorg Med Chem, 24 (6): (1356-1361). [PMID:26897091] |
103. Laufer R, Li SW, Liu Y, Ng G, Lang Y, Feher M, Brokx R, Beletskaya I, Hodgson R, Mao G, Plotnikova O, Awrey DE, Mason JM, Wei X, Lin DC, Che Y, Kiarash R, Madeira B, Fletcher GC, Mak TW, Bray MR, Pauls HW.. (2016) Discovery of 4-(4-aminopyrazolo[1,5-a][1,3,5]triazin-8-yl)benzamides as novel, highly potent and selective, orally bioavailable inhibitors of Tyrosine Threonine Kinase, TTK.. Bioorg Med Chem Lett, 26 (15): (3562-3566). [PMID:27335255] |
104. Kumar V, Guru SK, Jain SK, Joshi P, Gandhi SG, Bharate SB, Bhushan S, Bharate SS, Vishwakarma RA.. (2016) A chromatography-free isolation of rohitukine from leaves of Dysoxylum binectariferum: Evaluation for in vitro cytotoxicity, Cdk inhibition and physicochemical properties.. Bioorg Med Chem Lett, 26 (15): (3457-3463). [PMID:27363938] |
105. Kim H, Lee C, Yang JS, Choi S, Park CH, Kang JS, Oh SJ, Yun J, Kim MH, Han G.. (2016) Structural modifications at the 6-position of thieno[2,3-d]pyrimidines and their effects on potency at FLT3 for treatment of acute myeloid leukemia.. Eur J Med Chem, 120 (74-85). [PMID:27187860] |
106. Wurz RP, Sastri C, D'Amico DC, Herberich B, Jackson CLM, Pettus LH, Tasker AS, Wu B, Guerrero N, Lipford JR, Winston JT, Yang Y, Wang P, Nguyen Y, Andrews KL, Huang X, Lee MR, Mohr C, Zhang JD, Reid DL, Xu Y, Zhou Y, Wang HL.. (2016) Discovery of imidazopyridazines as potent Pim-1/2 kinase inhibitors.. Bioorg Med Chem Lett, 26 (22): (5580-5590). [PMID:27769621] |
107. Zhang L, Zhang Z, Chen F, Chen Y, Lin Y, Wang J.. (2016) Aromatic heterocyclic esters of podophyllotoxin exert anti-MDR activity in human leukemia K562/ADR cells via ROS/MAPK signaling pathways.. Eur J Med Chem, 123 (226-235). [PMID:27484511] |
108. Fu DJ, Zhang L, Song J, Mao RW, Zhao RH, Liu YC, Hou YH, Li JH, Yang JJ, Jin CY, Li P, Zi XL, Liu HM, Zhang SY, Zhang YB.. (2017) Design and synthesis of formononetin-dithiocarbamate hybrids that inhibit growth and migration of PC-3 cells via MAPK/Wnt signaling pathways.. Eur J Med Chem, 127 (87-99). [PMID:28038329] |
109. Cai Y, Li W, Tu H, Chen N, Zhong Z, Yan P, Dong J.. (2017) Curcumolide reduces diabetic retinal vascular leukostasis and leakage partly via inhibition of the p38MAPK/NF-κ B signaling.. Bioorg Med Chem Lett, 27 (8): (1835-1839). [PMID:28274631] |
110. Amin KM, Syam YM, Anwar MM, Ali HI, Abdel-Ghani TM, Serry AM.. (2017) Synthesis and molecular docking studies of new furochromone derivatives as p38α MAPK inhibitors targeting human breast cancer MCF-7 cells.. Bioorg Med Chem, 25 (8): (2423-2436). [PMID:28291685] |
111. Lim WC, Kim H, Kim YJ, Choi KC, Lee IH, Lee KH, Kim MK, Ko H.. (2017) Dioscin suppresses TGF-β1-induced epithelial-mesenchymal transition and suppresses A549 lung cancer migration and invasion.. Bioorg Med Chem Lett, 27 (15): (3342-3348). [PMID:28610976] |
112. Smith GP, Badolo L, Chell V, Chen IJ, Christensen KV, David L, Daechsel JA, Hentzer M, Herzig MC, Mikkelsen GK, Watson SP, Williamson DS.. (2017) The design and SAR of a novel series of 2-aminopyridine based LRRK2 inhibitors.. Bioorg Med Chem Lett, 27 (18): (4500-4505). [PMID:28802631] |
113. Fukuda T, Goto R, Kiho T, Ueda K, Muramatsu S, Hashimoto M, Aki A, Watanabe K, Tanaka N.. (2017) Discovery of DS79182026: A potent orally active hepcidin production inhibitor.. Bioorg Med Chem Lett, 27 (16): (3716-3722). [PMID:28705644] |
114. Fukuda T, Goto R, Kiho T, Ueda K, Muramatsu S, Hashimoto M, Aki A, Watanabe K, Tanaka N.. (2017) Discovery of DS28120313 as a potent orally active hepcidin production inhibitor: Design and optimization of novel 4,6-disubstituted indazole derivatives.. Bioorg Med Chem Lett, 27 (23): (5252-5257). [PMID:29079471] |
115. Gege C, Cummings MD, Albers M, Kinzel O, Kleymann G, Schlüter T, Steeneck C, Nelen MI, Milligan C, Spurlino J, Xue X, Leonard K, Edwards JP, Fourie A, Goldberg SD, Hoffmann T.. (2018) Identification and biological evaluation of thiazole-based inverse agonists of RORγt.. Bioorg Med Chem Lett, 28 (9): (1446-1455). [PMID:29631962] |
116. Diab S, Abdelaziz AM, Li P, Teo T, Basnet SKC, Noll B, Rahaman MH, Lu J, Hou J, Yu M, Le BT, Albrecht H, Milne RW, Wang S.. (2017) Dual Inhibition of Mnk2 and FLT3 for potential treatment of acute myeloid leukaemia.. Eur J Med Chem, 139 (762-772). [PMID:28863357] |
117. Bistrović A, Krstulović L, Harej A, Grbčić P, Sedić M, Koštrun S, Pavelić SK, Bajić M, Raić-Malić S.. (2018) Design, synthesis and biological evaluation of novel benzimidazole amidines as potent multi-target inhibitors for the treatment of non-small cell lung cancer.. Eur J Med Chem, 143 (1616-1634). [PMID:29133046] |
118. Liang C, Wu X, Li Z, Zhu J, Lu C, Shen Y.. (2018) Design, synthesis and pharmacological evaluation of N-(5-chloro-2,4-dihydroxybenzoyl)-(R)-N-arylmethyl-1,2,3,4-tetrahydro-3-isoquinolinecarboxamides as potent Hsp90 inhibitors.. Eur J Med Chem, 143 (85-96). [PMID:29172085] |
119. Reiersølmoen AC, Han J, Sundby E, Hoff BH.. (2018) Identification of fused pyrimidines as interleukin 17 secretion inhibitors.. Eur J Med Chem, 155 (562-578). [PMID:29909341] |
120. Kim SM, Park YJ, Shin MS, Kim HR, Kim MJ, Lee SH, Yun SP, Kwon SH.. (2017) Acacetin inhibits neuronal cell death induced by 6-hydroxydopamine in cellular Parkinson's disease model.. Bioorg Med Chem Lett, 27 (23): (5207-5212). [PMID:29089232] |
121. Li Q, Zhu ZX, Zhang X, Luo W, Chang LP, Chen S, Wang YX, Xie SQ, Chang CC, Wang CJ.. (2018) The lead optimization of the polyamine conjugate of flavonoid with a naphthalene motif: Synthesis and biological evaluation.. Eur J Med Chem, 146 (564-576). [PMID:29407981] |
122. Kaieda A, Takahashi M, Takai T, Goto M, Miyazaki T, Hori Y, Unno S, Kawamoto T, Tanaka T, Itono S, Takagi T, Hamada T, Shirasaki M, Okada K, Snell G, Bragstad K, Sang BC, Uchikawa O, Miwatashi S.. (2018) Structure-based design, synthesis, and biological evaluation of imidazo[1,2-b]pyridazine-based p38 MAP kinase inhibitors.. Bioorg Med Chem, 26 (3): (647-660). [PMID:29291937] |
123. Assadieskandar A, Yu C, Maisonneuve P, Liu X, Chen YC, Prakash GKS, Kurinov I, Sicheri F, Zhang C.. (2018) Effects of rigidity on the selectivity of protein kinase inhibitors.. Eur J Med Chem, 146 (519-528). [PMID:29407977] |
124. Wang Q, Liu F, Qi S, Qi Z, Yan XE, Wang B, Wang A, Wang W, Chen C, Liu X, Jiang Z, Hu Z, Wang L, Wang W, Ren T, Zhang S, Yun CH, Liu Q, Liu J.. (2018) Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia.. Eur J Med Chem, 150 (366-384). [PMID:29544149] |
125. Jiang JK, Huang X, Shamim K, Patel PR, Lee A, Wang AQ, Nguyen K, Tawa G, Cuny GD, Yu PB, Zheng W, Xu X, Sanderson P, Huang W.. (2018) Discovery of 3-(4-sulfamoylnaphthyl)pyrazolo[1,5-a]pyrimidines as potent and selective ALK2 inhibitors.. Bioorg Med Chem Lett, 28 (20): (3356-3362). [PMID:30227946] |
126. Wang B, Wu J, Wu Y, Chen C, Zou F, Wang A, Wu H, Hu Z, Jiang Z, Liu Q, Wang W, Zhang Y, Liu F, Zhao M, Hu J, Huang T, Ge J, Wang L, Ren T, Wang Y, Liu J, Liu Q.. (2018) Discovery of 4-(((4-(5-chloro-2-(((1s,4s)-4-((2-methoxyethyl)amino)cyclohexyl)amino)pyridin-4-yl)thiazol-2-yl)amino)methyl)tetrahydro-2H-pyran-4-carbonitrile (JSH-150) as a novel highly selective and potent CDK9 kinase inhibitor.. Eur J Med Chem, 158 (896-916). [PMID:30253346] |
127. Melo TRF, Kumkhaek C, Fernandes GFDS, Lopes Pires ME, Chelucci RC, Barbieri KP, Coelho F, Capote TSO, Lanaro C, Carlos IZ, Marcondes S, Chegaev K, Guglielmo S, Fruttero R, Chung MC, Costa FF, Rodgers GP, Dos Santos JL.. (2018) Discovery of phenylsulfonylfuroxan derivatives as gamma globin inducers by histone acetylation.. Eur J Med Chem, 154 (341-353). [PMID:29852459] |
128. Dodo K, Kuboki E, Shimizu T, Imamura R, Magarisawa M, Takahashi M, Tokuhiro T, Yotsumoto S, Asano K, Nakao S, Terayama N, Suda T, Tanaka M, Sodeoka M.. (2019) Development of a Water-Soluble Indolylmaleimide Derivative IM-93 Showing Dual Inhibition of Ferroptosis and NETosis.. ACS Med Chem Lett, 10 (9): (1272-1278). [PMID:31531196] |
129. Zhang Q, Hu X, Wan G, Wang J, Li L, Wu X, Liu Z, Yu L.. (2019) Discovery of 3-(((9H-purin-6-yl)amino)methyl)-4,6-dimethylpyridin-2(1H)-one derivatives as novel tubulin polymerization inhibitors for treatment of cancer.. Eur J Med Chem, 184 (111728-111728). [PMID:31610375] |
130. Narayan S, Ramisetti S, Jaiswal AS, Law BK, Singh-Pillay A, Singh P, Amin S, Sharma AK.. (2019) ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.. Eur J Med Chem, 161 (456-467). [PMID:30384048] |
131. Michalak B, Piwowarski JP, Granica S, Waltenberger B, Atanasov AG, Khan SY, Breuss JM, Uhrin P, Żyżyńska-Granica B, Stojakowska A, Stuppner H, Kiss AK.. (2019) Eupatoriopicrin Inhibits Pro-inflammatory Functions of Neutrophils via Suppression of IL-8 and TNF-alpha Production and p38 and ERK 1/2 MAP Kinases.. J Nat Prod, 82 (2): (375-385). [PMID:30653318] |
132. Wang Y, Dou X, Jiang L, Jin H, Zhang L, Zhang L, Liu Z.. (2019) Discovery of novel glycogen synthase kinase-3α inhibitors: Structure-based virtual screening, preliminary SAR and biological evaluation for treatment of acute myeloid leukemia.. Eur J Med Chem, 171 (221-234). [PMID:30925338] |
133. Huang JM, Huang FI, Yang CR.. (2019) Moscatilin Ameliorates Tau Phosphorylation and Cognitive Deficits in Alzheimer's Disease Models.. J Nat Prod, 82 (7): (1979-1988). [PMID:31291099] |
134. Wang X, Yu C, Wang C, Ma Y, Wang T, Li Y, Huang Z, Zhou M, Sun P, Zheng J, Yang S, Fan Y, Xiang R.. (2019) Novel cyclin-dependent kinase 9 (CDK9) inhibitor with suppression of cancer stemness activity against non-small-cell lung cancer.. Eur J Med Chem, 181 (111535-111535). [PMID:31376566] |
135. Zhao L, Li Y, Wang Y, Qiao Z, Miao Z, Yang J, Huang L, Tian C, Li L, Chen D, Yang S.. (2019) Discovery of 4H-Chromen-4-one Derivatives as a New Class of Selective Rho Kinase (ROCK) Inhibitors, which Showed Potent Activity in ex Vivo Diabetic Retinopathy Models.. J Med Chem, 62 (23): (10691-10710). [PMID:31693351] |
136. Jang J, Son JB, To C, Bahcall M, Kim SY, Kang SY, Mushajiang M, Lee Y, Jänne PA, Choi HG, Gray NS.. (2017) Discovery of a potent dual ALK and EGFR T790M inhibitor.. Eur J Med Chem, 136 (497-510). [PMID:28528303] |
137. Oukoloff K, Coquelle N, Bartolini M, Naldi M, Le Guevel R, Bach S, Josselin B, Ruchaud S, Catto M, Pisani L, Denora N, Iacobazzi RM, Silman I, Sussman JL, Buron F, Colletier JP, Jean L, Routier S, Renard PY.. (2019) Design, biological evaluation and X-ray crystallography of nanomolar multifunctional ligands targeting simultaneously acetylcholinesterase and glycogen synthase kinase-3.. Eur J Med Chem, 168 (58-77). [PMID:30798053] |
138. Jung O, Lee J, Lee YJ, Yun JM, Son YJ, Cho JY, Ryou C, Lee SY.. (2016) Timosaponin AIII inhibits migration and invasion of A549 human non-small-cell lung cancer cells via attenuations of MMP-2 and MMP-9 by inhibitions of ERK1/2, Src/FAK and β-catenin signaling pathways.. Bioorg Med Chem Lett, 26 (16): (3963-3967). [PMID:27422337] |
139. Jnawali HN, Jeon D, Jeong MC, Lee E, Jin B, Ryoo S, Yoo J, Jung ID, Lee SJ, Park YM, Kim Y.. (2016) Antituberculosis Activity of a Naturally Occurring Flavonoid, Isorhamnetin.. J Nat Prod, 79 (4): (961-969). [PMID:26974691] |
140. Piala AT, Akella R, Potts MB, Dudics-Giagnocavo SA, He H, Wei S, White MA, Posner BA, Goldsmith EJ.. (2016) Discovery of novel TAOK2 inhibitor scaffolds from high-throughput screening.. Bioorg Med Chem Lett, 26 (16): (3923-3927). [PMID:27426302] |
141. Abdelhafez OM, Ahmed EY, Abdel Latif NA, Arafa RK, Abd Elmageed ZY, Ali HI.. (2019) Design and molecular modeling of novel P38α MAPK inhibitors targeting breast cancer, synthesized from oxygen heterocyclic natural compounds.. Bioorg Med Chem, 27 (7): (1308-1319). [PMID:30792101] |
142. Zak M,Hanan EJ,Lupardus P,Brown DG,Robinson C,Siu M,Lyssikatos JP,Romero FA,Zhao G,Kellar T,Mendonca R,Ray NC,Goodacre SC,Crackett PH,McLean N,Hurley CA,Yuen PW,Cheng YX,Liu X,Liimatta M,Kohli PB,Nonomiya J,Salmon G,Buckley G,Lloyd J,Gibbons P,Ghilardi N,Kenny JR,Johnson A. (2019) Discovery of a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signaling.. Bioorg Med Chem Lett, 29 (12.0): (1522-1531). [PMID:30981576] |
143. Hamilton GL,Chen H,Deshmukh G,Eigenbrot C,Fong R,Johnson A,Kohli PB,Lupardus PJ,Liederer BM,Ramaswamy S,Wang H,Wang J,Xu Z,Zhu Y,Vucic D,Patel S. (2019) Potent and selective inhibitors of receptor-interacting protein kinase 1 that lack an aromatic back pocket group.. Bioorg Med Chem Lett, 29 (12.0): (1497-1501). [PMID:31000154] |
144. Zhu P,Qian J,Xu Z,Meng C,Liu J,Shan W,Zhu W,Wang Y,Yang Y,Zhang W,Zhang Y,Ling Y. (2020) Piperlonguminine and Piperine Analogues as TrxR Inhibitors that Promote ROS and Autophagy and Regulate p38 and Akt/mTOR Signaling.. J Nat Prod, 83 (10.0): (3041-3049). [PMID:33026807] |
145. Jiang X,Zhou J,Wang Y,Chen L,Duan Y,Huang J,Liu C,Chen Y,Liu W,Sun H,Feng F,Qu W. (2020) Rational design and biological evaluation of a new class of thiazolopyridyl tetrahydroacridines as cholinesterase and GSK-3 dual inhibitors for Alzheimer's disease.. Eur J Med Chem, 207 (112751-112751). [PMID:32950908] |
146. Jiang X,Zhou J,Wang Y,Liu X,Xu K,Xu J,Feng F,Sun H. (2021) PROTACs suppression of GSK-3β, a crucial kinase in neurodegenerative diseases.. Eur J Med Chem, 210 (112949-112949). [PMID:33097303] |
147. Tabti R,Lamoureux F,Charrier C,Ory B,Heymann D,Bentouhami E,Désaubry L. (2021) Development of prohibitin ligands against osteoporosis.. Eur J Med Chem, 210 (112961-112961). [PMID:33129591] |
148. Rojas-Prats E,Martinez-Gonzalez L,Gonzalo-Consuegra C,Liachko NF,Perez C,Ramírez D,Kraemer BC,Martin-Requero Á,Perez DI,Gil C,de Lago E,Martinez A. (2021) Targeting nuclear protein TDP-43 by cell division cycle kinase 7 inhibitors: A new therapeutic approach for amyotrophic lateral sclerosis.. Eur J Med Chem, 210 (112968-112968). [PMID:33139113] |
149. Yang J,Chen K,Zhang G,Yang QY,Li YS,Huang SZ,Wang YL,Yang W,Jiang XJ,Yan HX,Zhu JQ,Xiang R,Luo YF,Li WM,Wei YQ,Li LL,Yang SY. (2018) Structural optimization and structure-activity relationship studies of N-phenyl-7,8-dihydro-6H-pyrimido[5,4-b][1,4]oxazin-4-amine derivatives as a new class of inhibitors of RET and its drug resistance mutants.. Eur J Med Chem, 143 (1148-1164). [PMID:29133048] |
150. Kumar, S S and 5 more authors.. (1997) Novel homologues of CSBP/p38 MAP kinase: activation, substrate specificity and sensitivity to inhibition by pyridinyl imidazoles.. Biochemical and biophysical research communications, (27): [PMID:9207191] |
151. Goedert, M M, Cuenda, A A, Craxton, M M, Jakes, R R and Cohen, P P.. (1997) Activation of the novel stress-activated protein kinase SAPK4 by cytokines and cellular stresses is mediated by SKK3 (MKK6); comparison of its substrate specificity with that of other SAP kinases.. The EMBO journal, (16): [PMID:9218798] |
152. Wang, X S XS and 12 more authors.. (1997) Molecular cloning and characterization of a novel p38 mitogen-activated protein kinase.. The Journal of biological chemistry, (19): [PMID:9295308] |
153. Jiang, Y Y and 8 more authors.. (1997) Characterization of the structure and function of the fourth member of p38 group mitogen-activated protein kinases, p38delta.. The Journal of biological chemistry, (28): [PMID:9374491] |
154. Parker, C G CG and 10 more authors.. (1998) Identification of stathmin as a novel substrate for p38 delta.. Biochemical and biophysical research communications, (28): [PMID:9731215] |
155. Hu, M C MC, Wang, Y P YP, Mikhail, A A, Qiu, W R WR and Tan, T H TH.. (1999) Murine p38-delta mitogen-activated protein kinase, a developmentally regulated protein kinase that is activated by stress and proinflammatory cytokines.. The Journal of biological chemistry, (12): [PMID:10066767] |
156. Hale, K K KK, Trollinger, D D, Rihanek, M M and Manthey, C L CL.. (1999) Differential expression and activation of p38 mitogen-activated protein kinase alpha, beta, gamma, and delta in inflammatory cell lineages.. Journal of immunology (Baltimore, Md. : 1950), (1): [PMID:10201954] |
157. Herbison, C E CE and 5 more authors.. (1999) Structure and polymorphism of two stress-activated protein kinase genes centromeric of the MHC: SAPK2a and SAPK4.. DNA sequence : the journal of DNA sequencing and mapping, [PMID:10727080] |
158. Schoorlemmer, J J and Goldfarb, M M.. (2001) Fibroblast growth factor homologous factors are intracellular signaling proteins.. Current biology : CB, (15): [PMID:11378392] |
159. Knebel, A A, Morrice, N N and Cohen, P P.. (2001) A novel method to identify protein kinase substrates: eEF2 kinase is phosphorylated and inhibited by SAPK4/p38delta.. The EMBO journal, (15): [PMID:11500363] |
160. Buée-Scherrer, Valérie V and Goedert, Michel M.. (2002) Phosphorylation of microtubule-associated protein tau by stress-activated protein kinases in intact cells.. FEBS letters, (27): [PMID:11943212] |
161. Zhu, Shan S and 14 more authors.. (2002) Minocycline inhibits cytochrome c release and delays progression of amyotrophic lateral sclerosis in mice.. Nature, (2): [PMID:11986668] |
162. Feijoo, Carmen C, Campbell, David G DG, Jakes, Ross R, Goedert, Michel M and Cuenda, Ana A.. (2005) Evidence that phosphorylation of the microtubule-associated protein Tau by SAPK4/p38delta at Thr50 promotes microtubule assembly.. Journal of cell science, (15): [PMID:15632108] |
163. Pani, Elisabetta E and Ferrari, Stefano S.. () p38MAPK delta controls c-Myb degradation in response to stress.. Blood cells, molecules & diseases, [PMID:18006338] |
164. Zahedi, René P RP and 8 more authors.. (2008) Phosphoproteome of resting human platelets.. Journal of proteome research, [PMID:18088087] |
165. Zhou, Xiaoming X, Ferraris, Joan D JD, Dmitrieva, Natalia I NI, Liu, Yusen Y and Burg, Maurice B MB.. (2008) MKP-1 inhibits high NaCl-induced activation of p38 but does not inhibit the activation of TonEBP/OREBP: opposite roles of p38alpha and p38delta.. Proceedings of the National Academy of Sciences of the United States of America, (8): [PMID:18367666] |
166. Efimova, Tatiana T.. (2010) p38delta mitogen-activated protein kinase regulates skin homeostasis and tumorigenesis.. Cell cycle (Georgetown, Tex.), (1): [PMID:20090411] |
167. Ozawa, Shigeyuki S, Ito, Shin S, Kato, Yasumasa Y, Kubota, Eiro E and Hata, Ryu-Ichiro R.. (2010) Human p38 delta MAP kinase mediates UV irradiation induced up-regulation of the gene expression of chemokine BRAK/CXCL14.. Biochemical and biophysical research communications, (11): [PMID:20478268] |
168. Cuadrado, Ana A and Nebreda, Angel R AR.. (2010) Mechanisms and functions of p38 MAPK signalling.. The Biochemical journal, (1): [PMID:20626350] |
169. May-Dracka TL,Arduini R,Bertolotti-Ciarlet A,Bhisetti G,Brickelmaier M,Cahir-McFarland E,Enyedy I,Fontenot JD,Hesson T,Little K,Lyssikatos J,Marcotte D,McKee T,Murugan P,Patterson T,Peng H,Rushe M,Silvian L,Spilker K,Wu P,Xin Z,Burkly LC. (2018) Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity.. Bioorg Med Chem Lett, 28 (10): (1964-1971). [PMID:29636220] |