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Published on: November 22, 2024
7H-Pyrrolo[2,3-d]pyrimidine-4-amines as Potential Inhibitors of Plasmodium falciparum Calcium-Dependent Protein
Tswene D Seanego1,2, Hlamulo E Chavalala1,2, Hendrik H Henning1
1Molecular Sciences Institute School of Chemistry, University of the Witwatersrand, Private Bag 3, PO WITS, 2050, South Africa.
Abstract:
A series of pyrrolo[2,3-d]pyrimidines were designed in silico as potential bumped kinase inhibitors targeting P. falciparum calcium dependent protein kinase 4 (PfCDPK4), with the potential to inhibit PfCDPK1 based on earlier studies of the two kinases. A small series of these compounds were prepared and assessed for inhibitory activity against PfCDPK4 and PfCDPK1 in vitro. Four of the compounds displayed promising inhibitory activity against either PfCDPK4 (IC50 =0.210-0.530 μM), or PfCDPK1 (IC50 =0.589 μM). These data will enable optimisation of the molecular model to better predict inhibitory activity against PfCDPK4.
