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

Authors: Tripathi R.P.; Rastogi S.K.; Kundu B.; Saxena J.K.; M. Reddy V.J.; Srivastava S.K.; Chandra S.; Bhaduri A.P.

Source: Combinatorial Chemistry & High Throughput Screening, Volume 4, Number 3, May 2001 , pp. 237-234(8)

Publisher: Bentham Science Publishers

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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.

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

Language: English

Document Type: Review article

DOI: 10.2174/1386207013331084

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