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Inhibition of farnesyl protein transferase by new farnesyl phosphonate derivatives of phenylalanine

被引：11
作者：
Lamothe, M
Perrin, D
Blotieres, D
Leborgne, M
Gras, S
Bonnet, D
Hill, BT
Halazy, S
机构：
[1] CTR RECH PIERRE FABRE,DIV MED CHEM,F-81106 CASTRES,FRANCE
[2] CTR RECH PIERRE FABRE,CANCEROL DIV,F-81106 CASTRES,FRANCE
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 12期
关键词：
D O I：
10.1016/0960-894X(96)00238-7
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
New farnesyl phosphonate derivatives of phenylalanine have been prepared as inhibitors of farnesyl-protein transferase (FPT). Enzyme inhibition studies with bovine brain FPT and rat liver squalene synthase show that compound <(3a)under bar> is a new, potent and selective FPT inhibitor. Moreover, structural modifications from <(3a)under bar> have provided some useful information concerning the key structural subunits necessary for optimum and selective FPT inhibition. Copyright (C) 1996 Elsevier Science Ltd
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页码：1291 / 1296
页数：6
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