Synthesis of some pyrazole derivatives and preliminary investigation of their affinity binding to P-glycoprotein

被引：149
作者：
Manna, F
Chimenti, F
Fioravanti, R
Bolasco, A
Secci, D
Chimenti, P
Ferlini, C
Scambia, G
机构：
[1] Univ Roma La Sapienza, Dipartimento Studi Chim & Tecnol Sostanze Biologi, I-00185 Rome, Italy
[2] Univ Cattolica Sacro Cuore, Dipartimento Ostetricia & Ginecol, I-00168 Rome, Italy
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 20期
关键词：
anticancer; pyrazoline; P-glycoprotein;
D O I：
10.1016/j.bmcl.2005.05.067
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of substituted pyrazolines were synthesized and evaluated for their anticancer activity and for their ability to inhibit P-glycoprotein-mediated multidrug resistance by direct binding to a purified protein domain containing an ATP-binding site and a modulator interacting region. Compounds 2a and e have been found to bind to P-glycoprotein with greater affinity. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码：4632 / 4635
页数：4
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