Identification of Novel 2,4,5-Trisubstituted Pyrimidines as Potent Dual Inhibitors of Plasmodial <i>Pf</i> GSK3/ <i>Pf</i> PK6 with Activity against Blood Stage Parasites In Vitro
Kareem A. Galal, Anna Truong, Frank E. Kwarcinski, Chandi de Silva, Krisha Avalani, Tammy M. Havener, Michael E. Chirgwin, Eric M. Merten, Han Wee Ong, Caleb Willis, Ahmad Abdelwaly, Mohamed A. Helal, Emily R. Derbyshire, Reena Zutshi, David H. Drewry
Abstract
GSK3 inhibitors with antiplasmodial activity can be identified and can set the stage for further optimization efforts.
Topics & Concepts
ChemistryIC50In vitroKinaseDrug discoveryPharmacologyEC50BiochemistryBiologySignaling Pathways in DiseaseProtein Kinase Regulation and GTPase SignalingUbiquitin and proteasome pathways