Combinatorial Chemistry & High Throughput Screening · 2001 · 26 citations · 0 references
PharmacyBiochemistryMedicinal ChemistryDrug DesignDrug DiscoveryEnzymologyAntiparasitic PharmacologyBioconjugation ChemistryEnzyme InhibitionTopoisomerase InhibitorsAmino AcidsDna Topoisomerase Ii InhibitionGlycoconjugate SynthesisLead Compound OptimizationLead Compound ScreeningSynthetic Dna Library ConstructionTopoisomerase Ii FunctionTopoisomerase Ii Inhibitors
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.