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.

引用

页码：1521 / 1530

页数：10

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