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1. Discovery of 4-Amino and 4-Hydroxy-1-aroylindoles as Potent Tubulin Polymerization Inhibitors.

Author

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

Subjects
*ACETIC acid, *POLYMERIZATION, *CHEMICAL inhibitors, *COLCHICINE, *CELL lines, *PHARMACEUTICAL chemistry, *TUBULINS
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 26and 27with IC 50of 0.9 and 0.6 μM, respectively, exhibited antitubulin activity superior or comparable to that of colchicine and combretastatin A-4. They also showed antiproliferative activity with IC 50of 0.3−5.4 nM in a set of human cancer cell lines. [ABSTRACT FROM AUTHOR]

Published
2008
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