Identification of inhibitors of DNA topoisomerase II from a synthetic library of glycoconjugates
| Autor: | V. J. M. Reddy, J. K. Saxena, Rama Pati Tripathi, Amiya P. Bhaduri, S. Chandra, Sanjay K. Srivastava, Shiva K. Rastogi, Bijoy Kundu |
|---|---|
| Rok vydání: | 2001 |
| Předmět: |
Acid derivative
chemistry.chemical_classification Stereochemistry Glycoconjugate Organic Chemistry General Medicine Biology Computer Science Applications chemistry.chemical_compound DNA Topoisomerase II chemistry Biochemistry Drug Discovery Topoisomerase II Inhibitors Filarial parasite Identification (biology) Enzyme Inhibitors Lead compound Glycoconjugates DNA Gene Library |
| Zdroj: | Combinatorial chemistryhigh throughput screening. 4(3) |
| ISSN: | 1386-2073 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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