Synthesis and PKC isozyme surrogate binding of indothiolactam-V, a new thioamide analogue of tumor promoting indolactam-V

被引：15

作者：

Nakagawa, Y

Irie, K ^{[1
]}

Ohigashi, H

Hayashi, H

Wender, PA

机构：

[1] Kyoto Univ, Grad Sch Agr, Div Appl Life Sci, Sakyo Ku, Kyoto 6068502, Japan

[2] Univ Osaka Prefecture, Dept Appl Biol Chem, Sakai, Osaka 5998531, Japan

[3] Stanford Univ, Dept Chem, Stanford, CA 94305 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 18期

关键词：

D O I：

10.1016/S0960-894X(00)00411-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

To investigate the role of the amide group of (-)-indolactam-V (1) on PKC binding, we synthesized (-)-indothiolactam-V (2), a new thioamide analogue of 1, by microbial conversion using Streptomyces blastmyceticum. Compounds 2 and 1 showed similar binding affinities to conventional PKCs but 2 had lower affinities to novel PKCs, suggesting that novel PKCs recognize amide modifications more effectively than conventional PKCs. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：2087 / 2090

页数：4

共 24 条

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