Design and synthesis of Pfmrk inhibitors as potential antimalarial agents

Authors
Xiao, ZL Waters, NC Woodard, CL Li, ZY Li, PK
Citation
Zl. Xiao et al., Design and synthesis of Pfmrk inhibitors as potential antimalarial agents, BIOORG MED, 11(21), 2001, pp. 2875-2878
Citations number
13
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
21
Year of publication
2001
Pages
2875 - 2878
Database
ISI
SICI code
0960-894X(20011105)11:21<2875:DASOPI>2.0.ZU;2-R
Abstract
The synthesis and inhibitory activities of 10 potential inhibitors of Pfmrk , a Plasmodium falciparum cyclin-dependent protein kinase, are described. T he most potent inhibitor is a 3-phenyl-quinolinone compound with an IC50 va lue of 18 muM. It is the first compound reported to inhibit Pfmrk at the mi cro molar range. (C) 2001 Elsevier Science Ltd. All rights reserved.