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7H‐Pyrrolo[2,3‐d]pyrimidine‐4‐amines as potential inhibitors of Plasmodium falciparum calcium dependent protein kinases

Von Wiley-VCH zur Verfügung gestellt

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 ( Pf CDPK4), with the potential to inhibit Pf CDPK1 based on earlier studies of the two kinases. A small series of these compounds were prepared and assessed for inhibitory activity against Pf CDPK4 and Pf CDPK1 in vitro . Four of the compounds displayed promising inhibitory activity against either Pf CDPK4 (IC 50 = 0.210 - 0.530 µM), or Pf CDPK1 (IC 50 = 0.589 µM). These data will enable optimisation of the molecular model to better predict inhibitory activity against Pf CDPK4.

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