Design and synthesis of histone deacetylase inhibitors: the development of apicidin transition state analogs

被引：15

作者：

Colletti, SL ^{[1
]}

Myers, RW

Darkin-Rattray, SJ

Schmatz, DM

Fisher, MH

Wyvratt, MJ

Meinke, PT

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：

apicidin; side chain; transition state inhibitors; histone deacetylase;

D O I：

10.1016/S0040-4039(00)01366-6

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A four step degradation of the C8 ethyl ketone of apicidin provided a route to the C6 aldehyde intermediate and several mechanism-based transition state inhibitors of histone deacetylase. The compounds generated herein delineate the significance of apicidin's side chain, highlighted by the high affinity C8 aldehyde and C8-keto-9,10-epoxide analogs of apicidin. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：7837 / 7841

页数：5

共 14 条

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