title: Design and synthesis of Pfmrk inhibitors as potential antimalarial agents.
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.
authors.affiliation: Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA.
authors.forename: Z
authors.initials: Z
authors.lastname: Xiao
authors.forename: N C
authors.initials: NC
authors.lastname: Waters
authors.forename: C L
authors.initials: CL
authors.lastname: Woodard
authors.forename: Z
authors.initials: Z
authors.lastname: Li
authors.forename: P K
authors.initials: PK
authors.lastname: Li
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry*; D018844:Cyclin-Dependent Kinases; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry*; D010963:Plasmodium falciparum / Q000201:enzymology; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors*; D000095043:Cyclin-Dependent Kinase-Activating Kinase
chemical_list: D000962:Antimalarials; D004791:Enzyme Inhibitors; D017346:Protein Serine-Threonine Kinases; D018844:Cyclin-Dependent Kinases; D000095043:Cyclin-Dependent Kinase-Activating Kinase