从豆甾醇出发,通过3-位羟基及5-位双键保护,22-位双键臭氧化,得到3-乙酰氧基胆甾-5-烯-22-醛(4).化合物4进一步与氨基脲、氨基硫脲缩合得到22-降豆甾-22-含氮衍生物,合成物结构经NMR、IR及MS等技术手段进行了表征.并采用6种不同的肿瘤细胞,利用MTT法对合成物进行体外抗肿瘤活性研究,结果表明,具有22-缩氨硫脲基的化合物8具有很好的体外抗肿瘤活性,其对MGC 7901、Hela、SMMC 7404及CNE-2细胞的IC50值分别为10.5、11.6、8.7及11.9.
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