Biological activities of substituted trichostatic acid derivatives

被引：6

作者：

Charrier, Cedric ^{[1
]}

Roche, Joelle ^{[2
]}

Gesson, Jean-Pierre ^{[1
]}

Bertrand, Philippe ^{[1
]}

机构：

[1] Univ Poitiers, CNRS, UMR 6514, F-86022 Poitiers, France

[2] Univ Poitiers, CNRS, UMR 6187, Inst Physiol & Biol Cellulaires, F-86022 Poitiers, France

来源：

JOURNAL OF CHEMICAL SCIENCES | 2009年 / 121卷 / 04期

关键词：

Trichostatic acid; HDAC; inhibitor; HISTONE DEACETYLASE INHIBITORS; CRYSTAL-STRUCTURE; CANCER; DIFFERENTIATION; POTENT; SAHA; CHEMISTRY; MECHANISM; HOMOLOG; ANALOGS;

D O I：

10.1007/s12039-009-0056-1

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

New substituted trichostatic acid derivatives have been synthesized and evaluated for their biological activities towards the H661 non-small lung cancer cell line. These syntheses were achieved by alkylation of propiophenones to introduce the side chain with a terminal precursor of hydroxamic acid and aminobenzamide derivatives. The first fluorinated derivatives of trichostatic acid are described, such as 6-fluoro trichostatin A, with antiproliferative activities in the micromolar range and with histone deacetylase inhibitory activity.

引用

页码：471 / 479

页数：9

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