Synthesis and modeling study of (2S,5R,6R)- and (2S,5R,6S)-6-hydroxy-8-(1-decynyl)-benzolactam-V8 as protein kinase C modulators

被引：7

作者：

Wei, ZL

Sakamuri, S

Petukhov, PA

George, C

Lewin, NE

Blumberg, PM

Kozikowski, AP

机构：

[1] Georgetown Univ, Med Ctr, Dept Neurol, Drug Discovery Program, Washington, DC 20007 USA

[2] USN, Res Lab, Washington, DC 20375 USA

[3] NCI, Cellular Carcinogenesis & Tumor Promot Lab, Bethesda, MD 20892 USA

来源：

ORGANIC LETTERS | 2002年 / 4卷 / 13期

关键词：

D O I：

10.1021/ol026013u

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

[GRAPHICS] Both (2S,5R,6R)- and (2S,5R,6S)-6-hydroxy-8-(1-decynyl)benzolactam-V8 were designed and synthesized as PKC modulators. Biological assays reveal the (6R)-ligand to be 20-fold more potent than its (6S)-counterpart in binding to PKCalpha.

引用

页码：2169 / 2172

页数：4

共 36 条

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