National Center for
4M84: Calcium-dependent Protein Kinase 1 From Toxoplasma Gondii (tgcdpk1) In Complex With Inhibitor Uw1455
ACS Med Chem Lett (2014) 5 p.40-44» All references (3)
5-Aminopyrazole-4-carboxamide was used as an alternative scaffold to substitute for the pyrazolopyrimidine of a known "bumped kinase inhibitor" to create selective inhibitors of calcium-dependent protein kinase-1 from both Toxoplasma gondii and Cryptosporidium parvum. Compounds with low nanomolar inhibitory potencies against the target enzymes were obtained. The most selective inhibitors also exhibited submicromolar activities in T. gondii cell proliferation assays and were shown to be non-toxic to mammalian cells.