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

[摘要]：1-Aroylindoline, 1-aroyl-1,2,3,4-tetrahydroquinoline, and 1-aroylindole derivs., e.g., I and II, were synthesized and evaluated for anticancer activity. The 4-amino and 4-hydroxy-1-aroylindoles I and II, with IC50 of 0.9 and 0.6 mM, resp., exhibited antitubulin activity superior or comparable to that of colchicine and combretastatin A-4. They also showed antiproliferative activity with IC50 of 0.3-5.4 nM in a set of human cancer cell lines.

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