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目的:合成3β,5α,6β-三羟基雄甾-17β-衍生物并考察其体外抗癌活性,探讨17β-侧链对抗癌活性的影响。方法:以孕烯醇酮为原料经乙酰化、溴仿反应、甲酯化、过氧化氢氧化、水解、再分别进行乙酯化和丁酯化等步骤合成了4个目标化合物;以孕烯醇酮、醋酸去氢表雄酮和薯蓣皂素为原料经过氧化氢氧化等步骤合成了3个目标化合物;3β,5α,6β-三羟基孕甾-20-酮经格式反应等步骤合成2个目标化合物。采用MTT活细胞染色法,对目标化合物进行BEL-7402人肝癌细胞体外增殖抑制实验。结果:合成了9个目标化合物并经元素分析、IR和~1HNMR确证了结构。结论:L7,L11和L12对BEL-7402人肝癌细胞有一定的抗癌活性,L12抗癌活性最好。
OBJECTIVE: To synthesize 3β, 5α, 6β-trihydroxy-androsta-17β-derivatives and study their anticancer activity in vitro and to explore the effect of 17β-side chain on anticancer activity. Methods: Pregnenolone was used as raw material to synthesize 4 target compounds via acetylation, bromoform reaction, methyl esterification, hydrogen peroxide oxidation and hydrolysis, respectively. Aldosterone acetate, dehydroepiandrosterone acetate and diosgenin as raw materials through the oxidation of hydrogen peroxide and other steps to synthesize the 3 target compounds; 3β, 5α, 6β-trihydroxypregn-20-ketone by the format reaction step synthesis of 2 The target compound. MTT assay was used to detect the proliferation of BEL-7402 human hepatocellular carcinoma cells in vitro. Results: Nine target compounds were synthesized and confirmed by IR, ~ 1HNMR and elemental analysis. Conclusion: L7, L11 and L12 have certain antitumor activity against BEL-7402 human hepatoma cells, and L12 has the best anticancer activity.