一种新型强效柔红霉素酮衍生物的合成及其细胞毒性活性
Synthesis and cytotoxic activity of a new potent daunomycinone derivative.
作者信息
Aligiannis Nectarios, Pouli Nicole, Marakos Panagiotis, Skaltsounis Alexios-Leandros, Pratsinis Harris
机构信息
Division of Pharmacognosy, Department of Pharmacy, University of Athens, Panepistimiopolis-Zografou, Greece.
出版信息
Bioorg Med Chem Lett. 2002 Dec 16;12(24):3505-7. doi: 10.1016/s0960-894x(02)00823-5.
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.
描述了4'-叠氮基-3'-溴-3'-脱氨基-4'-脱氧柔红霉素的制备及其细胞毒性活性。发现该新化合物在体外对L1210以及敏感细胞系KB-3-1和MES-SA的活性低于阿霉素，但对阿霉素耐药亚系KB-A1和多药耐药MES-SA/Dx5亚系仍具有显著的细胞毒性。
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