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ID: ALA1136183

Journal: Bioorg Med Chem Lett

Title: Antitumor agents. Part 226: synthesis and cytotoxicity of 2-phenyl-4-quinolone acetic acids and their esters.

Authors: Xia Y, Yang ZY, Xia P, Bastow KF, Nakanishi Y, Nampoothiri P, Hamel E, Brossi A, Lee KH.

Abstract: 2-Phenyl-4-quinolone acetic acids and their esters were synthesized and evaluated for interaction with tubulin and for cytotoxicity against a panel of human tumor cell lines. 2-Phenyl- and 2-(2'-fluorophenyl)-4-quinolone-8-acetic acids (11 and 12) displayed potent cytotoxicity with ED(50) values at nanomolar concentrations, but had minimal activity against tubulin polymerization. 2-(2'-Fluorophenyl)-4-quinolone-6-acetic acid (3) and 2-(2'-fluorophenyl)-4-quinolone-8-acetic acid methyl ester (10) moderately inhibited tubulin polymerization.

CiteXplore: 14611851

DOI: 10.1016/s0960-894x(03)00624-3