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Identification of Inhibitors of DNA Topoisomerase II from a Synthetic Library of Glycoconjugates

[ Vol. 4 , Issue. 3 ]


R. P. Tripathi, S. K. Rastogi, B. Kundu, J. K. Saxena, V. J. M. Reddy, S. K. Srivastava, S. Chandra and A. P. Bhaduri   Pages 237 - 244 ( 8 )


A library of 24 glycoconjugates related to glycosylated b-amino acid derivative (I) was been prepared and screened against DNA topoisomerase-II of the filarial parasite S. cervi. Among these, compound 6 was found to be a potent inhibitor of DNA topoisomerase-II with 95percent inhibition at 1.0?mM. Furthermore, compound 6 was at least three times more potent than the lead compound, glycosylated b-amino acid derivative I.


DNA Topoisomerase II, filarial parasites, nalidixic acid, Fmoc-protected amino acids, propanoyl Sieber Amide Resin, negative ninhydrin test, Cys-Gly adornment


Divisions of Medicinal Chemistry, Central Drug Research Institute, Luckow.

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