Synthesis and cytotoxic activity of a new potent daunomycinone derivative.
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.
Aligiannis
Nectarios
N
Division of Pharmacognosy, Department of Pharmacy, University of Athens, Panepistimiopolis-Zografou, Greece.
Pouli
Nicole
N
Marakos
Panagiotis
P
Skaltsounis
Alexios-Leandros
AL
Pratsinis
Harris
H
D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000138:chemical synthesis / Q000494:pharmacology; D002241:Carbohydrates / Q000737:chemistry; D002455:Cell Division / Q000187:drug effects; D003630:Daunorubicin / Q000031:analogs & derivatives*; D004317:Doxorubicin / Q000494:pharmacology; D018432:Drug Resistance, Multiple; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D020128:Inhibitory Concentration 50; D051379:Mice; D009279:Naphthacenes / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D000903:Antibiotics, Antineoplastic; D002241:Carbohydrates; D009279:Naphthacenes; D004317:Doxorubicin; C019318:daunomycinone; D003630:Daunorubicin