非硫醇法尼基转移酶抑制剂：基于二苯甲酮的双底物类似物法尼基转移酶抑制剂的法尼基转移酶抑制作用及细胞活性

Non-thiol farnesyltransferase inhibitors: FTase-inhibition and cellular activity of benzophenone-based bisubstrate analogue farnesyltransferase inhibitors.

作者信息

Mitsch Andreas, Bergemann Silke, Gust Ronald, Sattler Isabel, Schlitzer Martin

机构信息

Institut für Pharmazeutische Chemie, Philipps-Universität Marburg, Marburg, Germany.

出版信息

Arch Pharm (Weinheim). 2003 Jul;336(4-5):242-50. doi: 10.1002/ardp.200300758.

DOI:10.1002/ardp.200300758

PMID:12916059

Abstract

Some 5-acylaminoacylamino-benzophenone derivatives were designed as bisubstrate analogue farnesyltransferase inhibitors. These compounds turned out to be only weakly active against farnesyltransferase, but displayed an antiproliferative effect rendering them suitable for further development as a novel type of cytostatic agents.

摘要

一些5-酰基氨基酰基氨基二苯甲酮衍生物被设计为双底物类似物法尼基转移酶抑制剂。结果发现这些化合物对法尼基转移酶的活性较弱，但具有抗增殖作用，使其适合作为新型细胞抑制剂进一步开发。