Synthesis and biological activity of 3'-deamino-3'-haloanthracyclines.

作者信息

Demetzos C, Skaltsounis A L, Michel S, Tillequin F, Koch M, Anstett M, Leonce S, Pierré A, Atassi G

机构信息

Laboratoire de Pharmacognosie de l'Université René Descartes, URA au CNRS No 1310, Faculté des Sciences Pharmaceutiques et Biologiques, Paris, France.

出版信息

Anticancer Drug Des. 1994 Apr;9(2):129-37.

4'-O-Acetyl-3'-deamino-3'-chloro and 4'-O-acetyl-3'-deamino-3'-bromoepidaunorubicin analogs have been synthesized by condensation of daunomycinone with the corresponding hexopyranosyl chlorides. The glycosides obtained were less potent than adriamycin (ADR) in inhibiting the proliferation of tumor cells in vitro, but they have shown promising activity against a variety of multidrug resistant (MDR) cell lines.