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肟醚类化合物往往表现出很好的杀虫、除草、抗菌、抗病毒以及抗肿瘤等生理活性,因而受到人们的广泛关注.从胆甾醇、豆甾醇出发,通过不同的合成路线,制备得到系列3-取代、6-取代及22-取代甲氧基肟醚和苄氧基肟醚甾体化合物,通过IR、NMR及MS等现代分析方法对合成物进行了结构表征.同时,分别采用人胃癌细胞(SGC-7901)、人肝癌细胞(Bel-7404)和鼻咽癌细胞(CNE-2)对合成产物及部分合成中间体进行了体外抑制肿瘤细胞生长增殖活性研究.结果表明,某些具有22-取代结构的甲氧肟醚及苄氧肟醚甾体化合物对这些肿瘤细胞株表现出较好的抑制活性,其中22-降-3β-羟基-22-苄氧肟基-豆甾-6-缩胺硫腙(15)对人鼻咽癌细胞CNE-2的IC50值为5.7μmol/L.
Oxime ethers are often concerned with their biocidal activities such as herbicidal activities, herbicidal activities, antimicrobial activities, antiviral activities and antitumor activities. Starting from cholesterol and stigmasterol, different series of synthetic routes have been prepared The 3-substituted, 6-substituted and 22-substituted methoxyoxime ethers and benzyloxyoxime ethers steroids were characterized by means of IR, NMR and MS.At the same time, human gastric cancer (SGC-7901), human hepatocellular carcinoma cell line (Bel-7404) and nasopharyngeal carcinoma cell line (CNE-2) on the synthesis of some synthetic intermediates and inhibition of tumor cell growth and proliferation activity of the results show that some have The 22-substituted methoxsone and benoxime ether steroid compounds showed good inhibitory activity against these tumor cell lines, among which, 22-nor-3β-hydroxy-22-benzyloxyhydroxy- -thiazinone (15) has an IC50 value of 5.7 μmol / L on human nasopharyngeal carcinoma cell line CNE-2.