Author/Authors :
Yi Xia، نويسنده , , Zhengyu Yang، نويسنده , , Peng-Xia Liu، نويسنده , , Kenneth F. Bastow، نويسنده , , Yuka Nakanishi، نويسنده , , Priya Nampoothiri، نويسنده , , Ernest Hamel، نويسنده , , Arnold Brossi، نويسنده , , Kuo-Hsiung Lee، نويسنده ,
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 ED50 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.