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

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

Volume: 4 Issue: 3

Author(s): R. P. Tripathi, S. K. Rastogi, B. Kundu, J. K. Saxena, V. J. M. Reddy, S. K. Srivastava, S. Chandra and A. P. Bhaduri

Affiliation:

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

Abstract: 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.

Cite this article as:

Tripathi P. R., Rastogi K. S., Kundu B., Saxena K. J., M. Reddy J. V., Srivastava K. S., Chandra S. and Bhaduri P. A., Identification of Inhibitors of DNA Topoisomerase II from a Synthetic Library of Glycoconjugates, Combinatorial Chemistry & High Throughput Screening 2001; 4 (3) . https://dx.doi.org/10.2174/1386207013331084