Structure-activity relationship study of 4-(thiazol-5-yl)benzoic acid derivatives as potent protein kinase CK2 inhibitors.
Basic Information
ID: ALA3758074
Journal: Bioorg Med Chem
Title: Structure-activity relationship study of 4-(thiazol-5-yl)benzoic acid derivatives as potent protein kinase CK2 inhibitors.
Authors: Ohno H, Minamiguchi D, Nakamura S, Shu K, Okazaki S, Honda M, Misu R, Moriwaki H, Nakanishi S, Oishi S, Kinoshita T, Nakanishi I, Fujii N.
Abstract: Two classes of modified analogs of 4-(thiazol-5-yl)benzoic acid-type CK2 inhibitors were designed. The azabenzene analogs, pyridine- and pyridazine-carboxylic acid derivatives, showed potent protein kinase CK2 inhibitory activities [IC50 (CK2α)=0.014-0.017μM; IC50 (CK2α')=0.0046-0.010μM]. Introduction of a 2-halo- or 2-methoxy-benzyloxy group at the 3-position of the benzoic acid moiety maintained the potent CK2 inhibitory activities [IC50 (CK2α)=0.014-0.016μM; IC50 (CK2α')=0.0088-0.014μM] and led to antiproliferative activities [CC50 (A549)=1.5-3.3μM] three to six times higher than those of the parent compound.
CiteXplore: 26850376
DOI: 10.1016/j.bmc.2016.01.043
Patent ID: ┄