Journal of medicinal and pharmaceutical chemistry 2008-07-24

Discovery of 4-amino and 4-hydroxy-1-aroylindoles as potent tubulin polymerization inhibitors.

Jing-Ping Liou, Zi-Yi Wu, Ching-Chuan Kuo, Chi-Yen Chang, Pei-Yi Lu, Chi-Ming Chen, Hsing-Pang Hsieh, Jang-Yang Chang

Index: J. Med. Chem. 51 , 4351, (2008)

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Abstract

1-Aroylindoline, 1-aroyl-1,2,3,4-tetrahydroquinoline, and 1-aroylindole derivatives were synthesized and evaluated for anticancer activity. The 4-amino and 4-hydroxy-1-aroylindoles 26 and 27 with IC 50 of 0.9 and 0.6 microM, respectively, exhibited antitubulin activity superior or comparable to that of colchicine and combretastatin A-4. They also showed antiproliferative activity with IC 50 of 0.3-5.4 nM in a set of human cancer cell lines.