Identification of inhibitors of DNA topoisomerase II from a synthetic library of glycoconjugates |
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| Authors: | Tripathi R P Rastogi S K Kundu B Saxena J K Reddy V J Srivastava S Chandra S Bhaduri A P |
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| Institution: | Division of Medicinal Chemistry, Central Drug Research Institute, Lucknow, 226 001, India. Bijoy_Kundu@Yahoo.com |
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| 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. |
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