Synthesis of side chain modified apicidin derivatives: potent mechanism-based histone deacetylase inhibitors

被引：29

作者：

Meinke, PT ^{[1
]}

Colletti, SL

Ayer, MB

Darkin-Rattray, SJ

Myers, RW

Schmatz, DM

Wyvratt, MJ

Fisher, MH

机构：

[1] Merck & Co Inc, Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA

[2] Merck & Co Inc, Merck Res Labs, Dept Parasite Biochem & Cell Biol, Rahway, NJ 07065 USA

来源：

TETRAHEDRON LETTERS | 2000年 / 41卷 / 41期

关键词：

histone deacetylase; apicidin; trapoxin; trichostatin; inhibitor; malaria;

D O I：

10.1016/S0040-4039(00)01364-2

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

An efficient degradation of apicidin's ketone-containing side chain to two common intermediates (the C7-aldehyde and the C8-methyl ester) is described. From these intermediates, a series of potent mechanism-based histone deacetylase inhibitors was prepared to facilitate biochemical studies. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：7831 / 7835

页数：5

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