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2005
Pyrimidine derivatives
R 0510
Syntheses of 2,4,6-Trisubstituted Pyrimidine Derivatives as a New Class of
Topoisomerase II Inhibitors. — A variety of new trisubstituted pyrimi15- 143 Antifilarial
dine derivatives (IX) (21 examples) are synthesized and evaluated for their in vitro
topoisomerase II inhibitory activity against filarial parasite Setaria cervi. Some of them,
e.g. (IXb) and (IXd), exhibit significant activity as compared to the standard
antifilarial drug DEC and topo II inhibitors novobiocin and nalidixic acid. —
(KATIYAR, S. B.; BANSAL, I.; SAXENA, J. K.; CHAUHAN*, P. M. S.; Bioorg.
Med. Chem. Lett. 15 (2005) 1, 47-50; Process Dev. Div., Cent. Drug Res. Inst.,
Lucknow 226 001, India; Eng.) — R. Langenstrassen
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