Table 1. Inhibition Profile of Alkynes against T. brucei*.
Compare compounds to 3, T. brucei EC50 = 0.26/0.4 μM. EC50 = 0.26 μM is obtained from our initial screening program with parasite concentration of 2 × 103 cells/mL, and for direct comparison with other compounds, 3 was retested in the same assays that its derivatives were tested in at 5 × 104 cells/mL (EC50 = 0.4 μM).
Ar is 3-chloro-4-((3-fluorobenzyl)oxy)phenyl.
Compounds showing >75% growth inhibition at 5 μM for T. brucei were tested for EC50 values. T. brucei EC50 values are the result of triplicate experiments.
SI is selectivity index = HepG2 TC50/Tbb EC50.
