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.