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© Yang SI, Institut Pasteur
Publication : Organic & biomolecular chemistry

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

Scientific Fields
Diseases
Organisms
Applications
Technique

Published in Organic & biomolecular chemistry - 18 Feb 2005

Duca M, Arimondo PB, Léonce S, Pierré A, Pfeiffer B, Monneret C, Dauzonne D

Link to Pubmed [PMID] – 15750651

Org. Biomol. Chem. 2005 Mar;3(6):1074-80

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.