title: Identification of inhibitors of DNA topoisomerase II from a synthetic library of glycoconjugates.
abstract: A library of 24 glycoconjugates related to glycosylated beta-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 95% inhibition at 1.09 microM. Furthermore, compound 6 was at least three times more potent than the lead compound, glycosylated beta-amino acid derivative I.
authors.affiliation: Division of Medicinal Chemistry, Central Drug Research Institute, Lucknow, 226 001, India. Bijoy_Kundu@Yahoo.com
authors.forename: R P
authors.initials: RP
authors.lastname: Tripathi
authors.forename: S K
authors.initials: SK
authors.lastname: Rastogi
authors.forename: B
authors.initials: B
authors.lastname: Kundu
authors.forename: J K
authors.initials: JK
authors.lastname: Saxena
authors.forename: V J
authors.initials: VJ
authors.lastname: Reddy
authors.forename: S
authors.initials: S
authors.lastname: Srivastava
authors.forename: S
authors.initials: S
authors.lastname: Chandra
authors.forename: A P
authors.initials: AP
authors.lastname: Bhaduri
mesh_terms: D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D015723:Gene Library; D006001:Glycoconjugates / Q000737:chemistry* / Q000494:pharmacology*; D059005:Topoisomerase II Inhibitors
chemical_list: D004791:Enzyme Inhibitors; D006001:Glycoconjugates; D059005:Topoisomerase II Inhibitors