α-双炔失碳醇类似物的合成及其抑制黄体细胞的生物活性

Synthesis and the Biological Activity of Inhibit Luteal Cells of Anordiol Analogues

目的:获得活性更高、副作用更小的抗生育甾体化合物。方法:以化合物A环失碳-17-羰基-5α-雄甾烷-2α乙炔基-2β-羟基为原料,通过对双炔失碳醇进行结构修饰,经数步反应得到各种含N或S基团的α-双炔失碳醇类似物,并对获得的新化合物进行体外黄体细胞抑制活性的生物试验。结果:合成了8个双炔失碳醇类似物,其体外生物活性试验结果显示,其中3个化合物的体外抑制黄体细胞生物活性高于双炔失碳醇。结论:双炔失碳醇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双炔失碳醇活性更高、副作用更小的甾体避孕药,值得进一步研究。

Objective： To obtain the higher activity and lower side effects of anti-fertility steroid compounds. Methods： A-nor-steroidal-17-carbonyl-5α-steranes-2α-acetylene-2β-hydroxy as raw materials, through the structural modification, anordiol analogues were synthesized. And the new compounds were screened with rat luteal cells in vitro bio-test. Results： Finally 8 new compounds were synthesized. Primary biological test showed that 3 compounds had much higher bioactivity than anordiol in vitro. Condusiou： Anordiol 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.