4-酰氧基黄体酮衍生物的合成及其细胞毒性

以黄体酮为前体，经4,5-环氧黄体酮合成了4-羟基黄体酮（2）; 2与酰氯经酰化反应合成了一系列新型4-酰氧基黄体酮衍生物（4a~4i），其结构经¹H NMR，¹³C NMR和MS（ESI）表征。体外细胞毒性实验结果表明：在用药量为50 μg·mL^-1时， 4c， 4d和4e对MCF-7细胞的抑制率分别为26%， 22%和13%。

Synthesis and Cytotoxicity of 4-Acyloxy Modified Derivatives from Progesterone

The 4-hydroxyprogesterone (2) was prepared from 4,5-epoxy progesterone , using progester-one as raw material.A series of novel 4-acyloxy progesterones (4a~4i) were synthesized by acetyla-tion reaction of 2 with different acyl chlorides (3a ~3i).The structures were characterized by 1H NMR, 13C NMR and MS(ESI).The in vitro cytotoxicity results showed that 4c, 4d and 4e exhibi-ted weak activity against the MCF-7 cells at the concentrations of 50 mg· mL-1 , with inhibition rate of 26%, 22%and 13%, respectively .