BISINDOLYLMALEIMIDE INHIBITORS OF PROTEIN-KINASE-C - FURTHER CONFORMATIONAL RESTRICTION OF A TERTIARY AMINE SIDE-CHAIN

被引：12

作者：

DAVIS, PD ^{[1
]}

HALLAM, TJ ^{[1
]}

HARRIS, W ^{[1
]}

HILL, CH ^{[1
]}

LAWTON, G ^{[1
]}

NIXON, JS ^{[1
]}

SMITH, JL ^{[1
]}

VESEY, DR ^{[1
]}

WILKINSON, SE ^{[1
]}

机构：

[1] ROCHE RES CTR,BROADWATER RD,WELWYN GARDEN CIT AL7 3AY,HERTS,ENGLAND

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1994年 / 4卷 / 11期

关键词：

D O I：

10.1016/S0960-894X(01)80349-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A pharmacophore model for the localisation of the cationic binding site of bisindolylmaleimide PKC inhibitors is described. This model has been used to guide selection of further conformationally restricted tertiary amine analogues, culminating in the identification and synthesis of the potent and highly selective PKC inhibitor, Ro 32-0557.

引用

页码：1303 / 1308

页数：6

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