Activities of pyrazolopyrimidine sulfamates as inhibitors of parasite growth.

P. falciparum (3D7, ring stage) cultures were exposed to different nucleoside sulfamates for 72 h and the 50% Inhibitory Concentration (IC50) for growth inhibition assessed using the lactate dehydrogenase (PfLDH) assay. Alternatively, synchronized Cam3.IIrev parasite cultures were subjected to 6-h pulses of nucleoside sulfamates, at the trophozoite (25–30 h.p.i.) stage. 50% growth inhibition (IC50) was determined in the cycle following treatment, using a SYBR Green I assay. HepG2 cell cultures were exposed to nucleoside sulfamates for 72 h and growth inhibition (IC50) assessed using CellTiter-Glo reagent. Data represent the mean of three independent experiments and error bars correspond to SEM. AMS = Adenosine 5’-sulfamate. n = Number of biological repeats. Medicines for Malaria Venture (MMV) designations for the compound names are in brackets.