作为潜在抗疟药物的Pfmrk抑制剂的设计与合成。
Design and synthesis of Pfmrk inhibitors as potential antimalarial agents.
作者信息
Xiao Z, Waters N C, Woodard C L, Li Z, Li P K
机构信息
Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA.
出版信息
Bioorg Med Chem Lett. 2001 Nov 5;11(21):2875-8. doi: 10.1016/s0960-894x(01)00578-9.
Abstract
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 IC(50) value of 18 microM. It is the first compound reported to inhibit Pfmrk at the micro molar range.
摘要
本文描述了恶性疟原虫细胞周期蛋白依赖性蛋白激酶Pfmrk的10种潜在抑制剂的合成及其抑制活性。最有效的抑制剂是一种3-苯基喹啉酮化合物，其IC(50)值为18微摩尔。它是首个被报道在微摩尔范围内抑制Pfmrk的化合物。
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