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

Author:

Galal Kareem A.1,Truong Anna2,Kwarcinski Frank3,de Silva Chandi3,Avalani Krisha3,Havener Tammy M.1ORCID,Chirgwin Michael E.2ORCID,Merten Eric1,Ong Han Wee1ORCID,Willis Caleb3,Abdelwaly Ahmad4,Helal Mohamed A.45ORCID,Derbyshire Emily R.26ORCID,Zutshi Reena3,Drewry David H.17ORCID

Affiliation:

1. Structural Genomics Consortium and Division of Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States

2. Department of Chemistry, Duke University, 124 Science Drive, Durham, North Carolina 27708, United States

3. Luceome Biotechnologies, L.L.C, 1665 E. 18th Street, Suite 106, Tucson, Arizona 85719, United States

4. Biomedical Sciences Program, University of Science and Technology, Zewail City of Science and Technology, Giza 12587, Egypt

5. Medicinal Chemistry Department, Faculty of Pharmacy, Suez Canal University, Ismailia 41522, Egypt

6. Department of Molecular Genetics and Microbiology, Duke University Medical Center, 213 Research Drive, Durham, North Carolina 27710, United States

7. Lineberger Comprehensive Cancer Center, Department of Medicine, School of Medicine, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States

Funder

Bayer

Merck KGaA

Genentech

Takeda Pharmaceutical Company

Bristol-Myers Squibb

Genome Canada

National Institutes of Health

Boehringer Ingelheim

Janssen Pharmaceuticals

National Science Foundation

Structural Genomics Consortium

EU/EFPIA/OICR/McGill/KTH/Diamond Innovative Medicines Initiative 2 Joint Undertaking

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

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