Activity of re-isolated compounds identified from the T.b. brucei primary and retest campaigns.

Species names are abbreviated. T.B = T.b. brucei; T.R = T.b rhodesiense; L.D = L. donovani; P.F = P. falciparum; T.C = T. cruzi.NA is not applicable as the IC50 value could not be determined within the dose range.(1)Compound numbers refer to those outlined in Figure 4.(2) SI was calculated with relative IC50 values of T.b. brucei and HEK293 cells. Value is described as “>” if the compound exhibited less than 50% activity at the top dose screened in the HEK293 assay at 75.8 µM, therefore an IC50 could not be estimated.(3)SI was calculated with relative IC50 values of T.b. rhodesiense, L. donovani, P. falciparum and T. cruzi to L6 cells.The standard deviation was calculated from two experiments with one replicate in each for the T. cruzi, L. donovani and P. falciparum assays and from three experiments containing two replicates each for the T.b. brucei assay.Compound activity against T. b. brucei and a panel of human infective protozoal species, including the HAT species T.b. rhodesiense of compounds identified from the T. b. brucei screening campaign. These compounds had the most favourable overall biological and medicinal chemistry profiles.