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PfCLK3 Inhibitors

Development of Potent PfCLK3 Inhibitors Based on TCMDC-135051 as a New Class of Antimalarials

August 17, 2020 - 13:13 -- Open Access
Author(s): 
Mahindra A, Janha O, Mapesa K, Sanchez-Azqueta A, Alam MM, Amambua-Ngwa A, Nwakanma DC, Tobin AB, Jamieson AG
Reference: 
J Med Chem. 2020 Aug 11

The protein kinase PfCLK3 plays a critical role in the regulation of malarial parasite RNA splicing and is essential for the survival of blood stage Plasmodium falciparum. We recently validated PfCLK3 as a drug target in malaria that offers prophylactic, transmission blocking, and curative potential. Herein, we describe the synthesis of our initial hit TCMDC-135051 (1) and efforts to establish a structure-activity relationship with a 7-azaindole-based series.

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