1. Discovery of 4-amino and 4-hydroxy-1-aroylindoles as potent tubulin polymerization inhibitors
- Author
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Chi Yen Chang, Ching Chuan Kuo, Zi Yi Wu, Jing Ping Liou, Pei Yi Lu, Hsing Pang Hsieh, Chi Ming Chen, and Jang Yang Chang
- Subjects
chemistry.chemical_classification ,Combretastatin ,Spectrometry, Mass, Electrospray Ionization ,Indoles ,Magnetic Resonance Spectroscopy ,biology ,Cell growth ,Stereochemistry ,Aromatic amine ,Chemical synthesis ,In vitro ,chemistry.chemical_compound ,Tubulin ,Biopolymers ,Biochemistry ,chemistry ,Cell culture ,Cell Line, Tumor ,Drug Discovery ,biology.protein ,Molecular Medicine ,Colchicine ,Humans - 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.
- Published
- 2008