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

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

Journal Name: Combinatorial Chemistry & High Throughput Screening
Accelerated Technologies for Biotechnology, Bioassays, Medicinal Chemistry and Natural Products Research

Volume 4 , Issue 3 , 2001

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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.

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

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Article Details

Year: 2001
Published on: 01 March, 2012
Page: [237 - 244]
Pages: 8
DOI: 10.2174/1386207013331084
Price: $65

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