Design and synthesis of Pfmrk inhibitors as potential antimalarial agents

被引：91
|
作者：
Xiao, ZL
Waters, NC
Woodard, CL
Li, ZY
Li, PK [1 ]
机构：
[1] Ohio State Univ, Coll Pharm, Div Med Chem & Pharmacognosy, Columbus, OH 43210 USA
[2] Walter Reed Army Inst Res, Div Expt Therapeut, Silver Spring, MD 20910 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 21期
关键词：
D O I：
10.1016/S0960-894X(01)00578-9
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The synthesis and inhibitory activities of 10 potential inhibitors of Pfmrk, a Plasmodium falciparum cyclin-dependent protein kinase, are described. The most potent inhibitor is a 3-phenyl-quinolinone compound with an IC50 value of 18 muM. It is the first compound reported to inhibit Pfmrk at the micro molar range. (C) 2001 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：2875 / 2878
页数：4
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