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Identification of Novel 2,4,5-Trisubstituted Pyrimidines as Potent Dual Inhibitors of Plasmodial PfGSK3/PfPK6 with Activity against Blood Stage Parasites In Vitro

[Image: see text] Essential plasmodial kinases PfGSK3 and PfPK6 are considered novel drug targets to combat rising resistance to traditional antimalarial therapy. Herein, we report the discovery of IKK16 as a dual PfGSK3/PfPK6 inhibitor active against blood stage Pf3D7 parasites. To establish struct...

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Detalles Bibliográficos
Autores principales: Galal, Kareem A., Truong, Anna, Kwarcinski, Frank, de Silva, Chandi, Avalani, Krisha, Havener, Tammy M., Chirgwin, Michael E., Merten, Eric, Ong, Han Wee, Willis, Caleb, Abdelwaly, Ahmad, Helal, Mohamed A., Derbyshire, Emily R., Zutshi, Reena, Drewry, David H.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2022
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9574854/
https://www.ncbi.nlm.nih.gov/pubmed/36166733
http://dx.doi.org/10.1021/acs.jmedchem.2c00996