SYNTHESIS AND BIOLOGICAL EVALUATION OF CONFORMATIONALLY CONSTRAINED BICYCLIC AND TRICYCLIC BALANOL ANALOGS AS INHIBITORS OF PROTEIN-KINASE-C

被引：29

作者：

MENDOZA, JS

JAGDMANN, GE

GOSNELL, PA

机构：

[1] Sphinx Pharmaceuticals, a Division of Eli Lilly and Company, Durham, NC 27707

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 19期

关键词：

D O I：

10.1016/0960-894X(95)00382-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of conformationally constrained bicyclic (20-25 and 28) and tricyclic (26 and 27) balanol analogues was prepared and evaluated as inhibitors of protein kinase C (PKC). Of special interest are bicyclic balanol analogues 20 and 24 and the tricyclic analogue 26, which not only retain the nanomolar activity for most PKC isozymes, but also display good selectivity over c-AMP dependent protein kinase (PKA).

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页码：2211 / 2216

页数：6

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