Novel carbamate derivatives of 4-beta-amino-4'-O-demethyl-4-desoxypodophyllotoxin as inhibitors of topoisomerase II: synthesis and biological evaluation |
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| Authors: | Duca Maria Arimondo Paola B Léonce Stéphane Pierré Alain Pfeiffer Bruno Monneret Claude Dauzonne Daniel |
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| Affiliation: | UMR 176 CNRS, Institut Curie, Section de Recherche, 26 rue d'Ulm, 75248 Paris cedex 05, France. |
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| Abstract: | A novel series of carbamate derivatives of 4-beta-amino-4'-O-demethyl-4-desoxypodophyllotoxin were synthesized. Their effect on human DNA topoisomerase II and antiproliferative activity was evaluated. Compounds 4a-c, 4g, 4j and 4k are topoisomerase II poisons that induce double-stranded breaks in DNA and exhibit increased cytotoxicity compared to etoposide. |
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