期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 52, 期 19, 页码 5916-5925出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm900476c
关键词
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资金
- Ministere de I'Education Superieure et de la Recherche
Several small weight indole derivatives (D-64131, D-24851, BPR0L075, BLF 61-3, and ATI derivatives) are potent tubulin polymerization inhibitors and show nanomolar antiproliferative activity. Among them, indolobenzazepin-7-ones were recently disclosed as potent antimitotic agents. In an effort to improve this structure, we prepared new derivatives in order to evaluate their antiproliferative activity. 5,6,7,9-Tetrahydro-8H-indolo[2,3-e][3]benzazocin-g-one (1m) was found to be the most potent derivative inhibiting the cell growth of several cancer cell lines in the lower nanomolar range.
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