Indolobenzazepin-7-ones and 6-, 8-, and 9-membered ring derivatives as tubulin polymerization inhibitors: synthesis and structure--activity relationship studies. - Archive ouverte HAL
Article Dans Une Revue Journal of Medicinal Chemistry Année : 2009

Indolobenzazepin-7-ones and 6-, 8-, and 9-membered ring derivatives as tubulin polymerization inhibitors: synthesis and structure--activity relationship studies.

Résumé

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-8-one (1m) was found to be the most potent derivative inhibiting the cell growth of several cancer cell lines in the lower nanomolar range.

Domaines

Chimie organique
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Dates et versions

hal-00691446 , version 1 (26-04-2012)

Identifiants

Citer

Aurélien Putey, Florence Popowycz, Quoc-Tuan Do, Philippe Bernard, Sandeep K Talapatra, et al.. Indolobenzazepin-7-ones and 6-, 8-, and 9-membered ring derivatives as tubulin polymerization inhibitors: synthesis and structure--activity relationship studies.. Journal of Medicinal Chemistry, 2009, 52 (19), pp.5916-25. ⟨10.1021/jm900476c⟩. ⟨hal-00691446⟩
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