Novel carbamate derivatives of 4-β-amino-4′-O-demethyl-4-desoxypodophyllotoxin as inhibitors of topoisomerase II: synthesis and biological evaluation,10.1039/B416862C

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Novel carbamate derivatives of 4-β-amino-4′-O-demethyl-4-desoxypodophyllotoxin as inhibitors of topoisomerase II: synthesis and biological evaluation

Paola B. Arimondo,Stéphane Léonce,Alain Pierré,Bruno Pfeiffer,Claude Monneret,Daniel Dauzonne

Organic & Biomolecular Chemistry Pub Date : 02/18/2005 00:00:00 , DOI:10.1039/B416862C

Abstract

A novel series of carbamate derivatives of 4-β-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.