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环硫雄醇的合成与药理研究
Synthesis and Pharmacological Studies of Epitiostanol
【摘要】 本文简述了环硫雄醇9的改良合成法及其四个衍生物的制备(其中两个为新合成化合物),并从溴羟化产物中用分级结晶法分离得主要副产物2β─溴─3α─羟基─5α──雄甾─17─酮6,又以6为起始原料合成2β,3β─环硫─5α─雄甾─17β─醇13。环硫雄醇9经药理及毒性试验表明具。有强烈抑制人乳腺癌(Bcap-37)和子宫颈癌(HeLa)细胞生长的作用;对小鼠有抗着床作用;且毒性低,副作用小。
【Abstract】 An improved method for the synthesis of EPITIOSTANOL and the prepara- tion of its four derivatives(including two new compounds )has been reported in this paper. The main by-product, 2β-bromo-3α-hydroxy-5α-androstan-17-one 6, was isolated as a bromohydrin by grade crystals method, and was then converted to 2β, 3β-Epithio-5α-androstan-17β-ol13. Studies on the pharmacological action and toxicity of EPITIOSTANOL have shown that it strongly inhibits the cell growth of breast cancer(Bcap-37)and cervical cancer(HeLa) and further more, it has anti-gestation, low toxin and less side effect.
【Key words】 anti-estrogen; antitumor agents; anti-gestation; contraceptives; bro-mohydrin;
- 【文献出处】 福州大学学报(自然科学版) ,Journal of Fuzhou University(Natural Sciences Edtion) , 编辑部邮箱 ,1988年03期
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