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环硫雄醇的合成与药理研究

Synthesis and Pharmacological Studies of Epitiostanol

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【作者】 李志达郭文璟陈振荣何长云潘秀森黄自强吴德丰李常春

【Author】 Li Zhida (Department of Chemistry) Guo Wenjing, Chen Zhenrong, He Changyun (Fuzhou Institute of Pharmaceutical Industry) Pan Xiusen, Huang Ziqiang, Wu Defeng, Li Changchun (Fujian Medical College)

【机构】 福州大学化学系福州市医药工业研究所福建医学院福建医学院

【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.

  • 【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
  • 【下载频次】61
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