柔红霉素和阿霉素自旋标记衍生物的合成与抗肿瘤活性

Synthesis and Antitumor Activities of Spin Labeled Derivatives of Daunorubicin and Doxorubicin

合成了 5个新的柔红霉素及阿霉素的氮氧自由基自旋标记衍生物 ( 5_ 9) ,经元素分析 ,IR,MS和ESR分析确证了其组成和结构 ,并对它们进行了抑制小鼠白血病 P3 88、小鼠黑色素癌 B1 6、人胃腺癌 MGC和人肝癌 SMMC772 1细胞的体外筛选 .初步药理试验表明 ,化合物 5_ 9对 4种瘤株均有一定的抑制活性 ,其中化合物

Five new spin labeled derivatives of daunorubicin and doxorubicin(5_9) were synthesized and their structures were identified by IR, MS and ESR as well as elementary analysis. All new compounds were evaluated for their antitumor activities against mouse leukemia P388, B16, human stomach carcinoma SGC 7901 and human liver cancer SMMC 7721 cells in vitro. The preliminary results showed that compound 9 was as active as the clinically used doxorubicin. [WT5HZ]