Potent and selective PKC inhibitory 5-membered ring analogs of balanol with replacement of the carboxamide moiety

被引：21

作者：

Jagdmann, GE

Defauw, JM

Lampe, JW

Darges, JW

Kalter, K

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 15期

关键词：

D O I：

10.1016/0960-894X(96)00311-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Balanol ((-)-1) is a potent protein kinase inhibitory natural product isolated from the fungus Verticillium balanoides. The lack of cellular activity and protein kinase C selectivity in balanol has prompted a search for analogs that incorporate these properties, This paper describes the synthesis and biological activity of such compounds with substitution similar to balanol, but with a single atom bridge in place of the carboxamide moiety. Copyright (C) 1996 Elsevier Science Ltd

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页码：1759 / 1764

页数：6

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