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

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.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Liou JP,Wu ZY,Kuo CC,Chang CY,Lu PY,Chen CM,Hsieh HP,Chang JY

doi

10.1021/jm800150d

subject

Has Abstract

pub_date

2008-07-24 00:00:00

pages

4351-5

issue

14

eissn

0022-2623

issn

1520-4804

journal_volume

51

pub_type

杂志文章

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