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Design and synthesis of Pfmrk inhibitors as potential antimalarial agents
Z Xiao1, N C Waters, C L Woodard
1Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA.
Bioorganic & Medicinal Chemistry Letters
|October 13, 2001
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.