Bioorganic and Medicinal Chemistry Letters p. 5264 - 5267 (2012)
Update date:2022-08-03
Topics:
Zhang, Zhongsheng
Ojo, Kayode K.
Johnson, Steven M.
Larson, Eric T.
He, Penqing
Geiger, Jennifer A.
Castellanos-Gonzalez, Alejandro
White Jr., A. Clinton
Parsons, Marilyn
Merritt, Ethan A.
Maly, Dustin J.
Verlinde, Christophe L.M.J.
Van Voorhis, Wesley C.
Fan, Erkang
Calcium-dependent protein kinase-1 (CDPK1) from Cryptosporidium parvum (CpCDPK1) and Toxoplasma gondii (TgCDPK1) have become attractive targets for discovering selective inhibitors to combat infections caused by these protozoa. We used structure-based design to improve a series of benzoylbenzimidazole-based compounds in terms of solubility, selectivity, and potency against CpCDPK1 and TgCDPK1. The best inhibitors show inhibitory potencies below 50 nM and selectivity well above 200-fold over two human kinases with small gatekeeper residues.
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(2012)