摘要
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 the higher activity and lower side effects of anti-fertility steroid compounds through the structural modification of dienogest.Methods： The estra-5（10）,9（11）-diene-3,17-dione-3,3-ethyleneketal as raw materials,7 compounds that contain N or S groups of dienogest anologues were synthesized.And the new compounds were screened with rat luteal cells in vitro bio-test.Result： Primary biological test showed that 2 compounds had much higher bioactivity than dienogest in vitro.Conclusion： Dienogest analogs that are reconstructed by us still possess excellent in vitro bioactivity,which suggests that further studies shall be carried out on this category of compounds.
出处
《生殖与避孕》
CAS
CSCD
2012年第1期5-9,共5页
Reproduction and Contraception
关键词
地诺孕素
结构改造
黄体细胞
dienogest
structural modification
luteal cells
