Design and synthesis of Pfmrk inhibitors as potential antimalarial agents |
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Authors: | Xiao Z Waters N C Woodard C L Li Z Li P K |
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Institution: | Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA. |
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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. |
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