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

…, I Bansal, JK Saxena, PMS Chauhan

Index: Katiyar, Sanjay Babu; Bansal, Iti; Saxena; Chauhan Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 1 p. 47 - 50

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Citation Number: 45

Abstract

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, seven compounds (8, 11–14, 25 and 28) have shown 60–80% inhibition at 40 and 20μg/mL concentration. Five compounds (12, 13, 14, 25 and 28) exhibited 70–80% inhibition at 10μg/mL concentration and three compounds (13, 14 and ...