Non-thiol farnesyltransferase inhibitors:: Structure-activity relationships of benzophenone-based bisubstrate analogue farnesyltransferase inhibitors

被引：19

作者：

Schlitzer, M

Böhm, M

Sattler, I

机构：

[1] Univ Marburg, Inst Pharmazeut Chem, D-35032 Marburg, Germany

[2] Hans Knoll Inst Nat Stoff Forsch EV, D-07745 Jena, Germany

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2002年 / 10卷 / 03期

关键词：

D O I：

10.1016/S0968-0896(01)00312-1

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：

Investigations on the structure-activity relationships of benzophenone-based bisubstrate analogue farnesyltransferase inhibitors yielded a bisubstrate analogue farnesyltransferase inhibitor lacking any prenylic or peptidic substructures with nanomolar activity. This represents a considerable progress in comparison to those non-prenylic, non-peptidic bisubstrate analogue farnesyltransferase inhibitors we have described before which utilized AAX-peptidomimetic substructures different from the benzophenone since those inhibitors displayed activity only in the micromolar range. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：615 / 620

页数：6

共 31 条

[1] Farnesyltransferase inhibitors and cancer treatment: targeting simply Ras? [J].