Synthesis and evaluation of isatin analogs as caspase-3 inhibitors: Introduction of a hydrophilic group increases potency in a whole cell assay

被引：40

作者：

Chu, Wenhua ^{[1
]}

Rothfuss, Justin ^{[1
]}

Zhou, Dong ^{[1
]}

Mach, Robert H. ^{[1
]}

机构：

[1] Washington Univ, Sch Med, Dept Radiol, Div Radiol Sci, St Louis, MO 63110 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 08期

基金：

美国国家卫生研究院;

关键词：

Caspase-3; Apoptosis; Cell death; SELECTIVE NONPEPTIDE INHIBITORS; SULFONAMIDE ANALOGS; 5-PYRROLIDINYLSULFONYL ISATINS; IN-VIVO; APOPTOSIS; DEATH; ACTIVATION; LIFE;

D O I：

10.1016/j.bmcl.2011.03.015

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of isatin analogs containing a hydrophilic group, including a pyridine ring, ethylene glycol group, and a triazole ring, have been synthesized, and their inhibition potency for caspase-3 was measured both in vitro (i.e., recombinant enzyme) and in whole cells (HeLa cells). The analogs having a hydrophilic group, including 12, 13, 16, 38, and 40, have dramatically increased activity in vitro and in HeLa cells compared to the corresponding unsubstituted N-phenyl isatin analogs. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：2192 / 2197

页数：6

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