蒽环类抗生素方形酸酰胺的形成。合成及细胞毒性特性。
Formation of squaric acid amides of anthracycline antibiotics. Synthesis and cytotoxic properties.
作者信息
Tevyashova Anna, Sztaricskai Ferenc, Batta Gyula, Herczegh Pál, Jeney András
机构信息
Research Group for Antibiotics of the Hungarian Academy of Sciences, and Department of Pharmaceutical Chemistry, University of Debrecen, Debrecen, PO Box 70, H-4010 Hungary.
出版信息
Bioorg Med Chem Lett. 2004 Sep 20;14(18):4783-9. doi: 10.1016/j.bmcl.2004.06.072.
The reaction of the anthracycline glycoside antibiotics 1-3 with the squaric acid ester 4 gave the squaric acid amide esters 5-7 under neutral conditions, whereas over pH7 the products are the symmetric diamides (8, 9, 11, and 12). Of the prepared compounds 11 was the most active on MCF-7 human mammary adenocarcinoma cells.
蒽环类糖苷抗生素1 - 3与方酸酯4在中性条件下反应生成方酰胺酯5 - 7，而在pH值大于7时，产物为对称二酰胺（8、9、11和12）。在所制备的化合物中，11对MCF - 7人乳腺腺癌细胞的活性最强。
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