Bioorganic & Medicinal Chemistry Letters 2002-12-16

Synthesis and cytotoxic activity of a new potent daunomycinone derivative.

Nectarios Aligiannis, Nicole Pouli, Panagiotis Marakos, Alexios-Leandros Skaltsounis, Harris Pratsinis

Index: Bioorg. Med. Chem. Lett. 12(24) , 3505-7, (2002)

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Abstract

The preparation and cytotoxic activity of 4'-azido-3'-bromo-3'-deamino-4'-deoxydaunorubicin is described. The new compound was found to be less active in vitro than adriamycin against L1210 and the sensitive cell lines KB-3-1 and MES-SA, but retained interesting cytotoxicity against the adriamycin resistant subline KB-A1 and the multidrug resistant MES-SA/Dx5 subline.