ID: ALA1147634
Journal: Bioorg Med Chem Lett
Title: Discovery of novel heteroaryl-substituted chalcones as inhibitors of TNF-alpha-induced VCAM-1 expression.
Authors: Meng CQ, Zheng XS, Ni L, Ye Z, Simpson JE, Worsencroft KJ, Hotema MR, Weingarten MD, Skudlarek JW, Gilmore JM, Hoong LK, Hill RR, Marino EM, Suen KL, Kunsch C, Wasserman MA, Sikorski JA.
Abstract: Novel chalcone derivatives have been discovered as potent inhibitors of TNF-alpha-induced VCAM-1 expression. Thienyl or benzothienyl substitution at the meta-position of ring B helps boost potency while large substitution at the para-position on ring B is detrimental. Various substitutions are tolerated on ring A. A lipophilicity-potency relationship has been observed in several sub-series of compounds.
CiteXplore: 15006393
DOI: 10.1016/j.bmcl.2004.01.021
Patent ID: ┄