Non-thiol farnesyltransferase inhibitors:: N-(4-acylamino-3-benzoylphenyl)-3-[5-(4-nitrophenyl)-2-furyl]acrylic acid amides

被引：13
作者：
Kettler, K
Sakowski, J
Silber, K
Sattler, I
Klebe, G
Schlitzer, M
机构：
[1] Univ Munich, Dept Pharm, D-81377 Munich, Germany
[2] Univ Marburg, Inst Pharmazeut Chem, D-35032 Marburg, Germany
[3] Hans Knoll Inst Naturstoff Forsch EV, D-07745 Jena, Germany
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2003年 / 11卷 / 07期
关键词：
D O I：
10.1016/S0968-0896(03)00064-6
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：
We have designed the nitrophenylfurylacryl-substituted benzophenone 4f as a non-thiol farnesyltransferase inhibitor utilizing a novel aryl binding site of farnesyltransferase. Variation of the 2-acylamino substituent at the benzophenone core structure of our initial lead 4f yielded several non-thiol farnesyltransferase inhibitors with improved activity. These compounds display activity in the low nanomolar range. (C) 2003 Elsevier Science Ltd. All rights reserved.
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页码：1521 / 1530
页数：10
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