Design of new inhibitors for CDC2 kinase based on a multiple pseudosubstrate structure

被引：15

作者：

Sasaki, S ^{[1
]}

Hashimoto, T

Obana, N

Yasuda, H

Uehara, Y

Maeda, A

机构：

[1] Kyushu Univ, Fac Pharmaceut Sci, Fukuoka 8128582, Japan

[2] Tokyo Univ Pharm & Life Sci, Sch Life Sci, Hachioji, Tokyo 19203, Japan

[3] Natl Inst Infect Dis, Tokyo 162, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 09期

关键词：

D O I：

10.1016/S0960-894X(98)00163-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

New inhibitors have been designed for cdc2 kinase based on a multiple pseudosubstrate structure. The new inhibitors have three different structural components: 3,4-bis(indol-3-yl)maleimide, Ac-Cys-(Ser)-Pro-Lys-Lys-NHMe, and ethyloxy group between the two components. Inhibitory activities toward cdc2 and other protein kinases were investigated, and the compound (21) with Ac-Cys-Pro-Lys-Lys-NHMe connected with the triethylene glycol spacer exhibited the most potent inhibition with relatively high selectivity. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：1019 / 1022

页数：4

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