Design, synthesis, and biological evaluation of a potent, PKC selective, B-ring analog of bryostatin

被引：31

作者：

Wender, PA ^{[1
]}

Verma, VA

机构：

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

[2] Stanford Univ, Dept Mol Pharmacol, Stanford, CA 94305 USA

来源：

ORGANIC LETTERS | 2006年 / 8卷 / 09期

关键词：

D O I：

10.1021/ol060457z

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The first member of a new class of five-membered B-ring analogs of bryostatin has been synthesized and tested for its ability to bind and translocate protein kinase C (PKC). This synthesis extends the utility of our previously introduced macrotransacetalization strategy to the formation of five-membered dioxolane B-ring analogs. This analog exhibits potent, single-digit nanomolar affinity to PKC and selectively translocates novel PKC isozymes.

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页码：1893 / 1896

页数：4

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