Discovery of novel nonpeptide tricyclic inhibitors of Ras farnesyl protein transferase

被引：40

作者：

Njoroge, FG

Doll, RJ

Vibulbhan, B

Alvarez, CS

Bishop, WR

Petrin, J

Kirschmeier, P

Carruthers, NI

Wong, JK

Albanese, MM

Piwinski, JJ

Catino, J

Girijavallabhan, V

Ganguly, AK

机构：

[1] SCHERING PLOUGH CORP,RES INST,DEPT CHEM,KENILWORTH,NJ 07033

[2] SCHERING PLOUGH CORP,RES INST,DEPT TUMOR BIOL,KENILWORTH,NJ 07033

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 1997年 / 5卷 / 01期

关键词：

D O I：

10.1016/S0968-0896(96)00206-4

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A comprehensive structure-activity relationship (SAR) study of novel tricyclic amides has been undertaken. The discovery of compounds that are potent FPT inhibitors in the nanomolar range has been achieved. These compounds are nonpeptidic and do not contain sulfhydryl groups. They selectively inhibit farnesyl protein transferase (FPT) and not geranylgeranyl protein transferase-1 (GGPT-1). They also inhibit H-Ras processing in Cos monkey kidney cells. Copyright (C) 1997 Elsevier Science Ltd.

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页码：101 / 113

页数：13

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