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.
引用
收藏
页码：1893 / 1896
页数：4
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