Syntheses of 2,4,6-trisubstituted pyrimidine derivatives as a new class of antifilarial topoisomerase II inhibitors

A series of 21 compounds of trisubstituted pyrimidine derivatives have been synthesized and evaluated for their in vitro topoisomerase II inhibitory activity against filarial parasite Setaria cervi. Out of these, five compounds (12, 13, 14, 25 and 28) exhibited 70-80% inhibition at 10 μg/mL and three compounds (13, 14 and 28) have shown 40-60% inhibition at 5 μg/mL concentration.