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目的:通过对地诺孕素进行结构改造,获得活性更高、副作用更小的抗生育甾体化合物。方法:以合成米非司酮的中间体3-(1’,3’-二氧戊环)-5(10),9(11)-雌甾二烯-17-酮为原料,合成7个含N或S基团的地诺孕素类似物,并进行体外黄体细胞抑制活性的生物试验。结果:体外生物活性试验结果显示,其中2个化合物的体外抑制黄体细胞生物活性高于地诺孕素。结论:地诺孕素的分子结构经改造后仍具有优良的体外生物活性,提示有可能从这一类结构特征的化合物中得到比地诺孕素活性更高的甾体避孕药,值得进一步研究。
OBJECTIVE: To obtain anti-fertility steroid compounds with higher activity and fewer side effects by structural modification of dienogestrel. Methods: The synthesis of mifepristone intermediates 3- (1 ’, 3’-dioxolan) -5 (10), 9 (11) -estradiol-17- Adenorbine analogs containing N or S groups and a biological assay of in vitro luteal cell inhibitory activity. Results: In vitro biological activity test results showed that two of the compounds in vitro inhibited the luteal cell biological activity than dronedin. CONCLUSION: The molecular structure of dienogestrel still has excellent biological activity after in vitro modification, suggesting that it is possible to obtain steroid contraceptives with higher activity than that of dienogestrel from the compounds with structural features of this class, which deserves further study .