多羟基甾醇的合成及其结构与抗肿瘤细胞活性关系研究

Synthesis of Some Polyhydroxysterols and Investigation of Relationship Between Their Structure and Cytotoxicity

报道了 6个具有类似结构的多羟基甾醇的合成和它们的抗肿瘤细胞活性 .发现此类化合物的细胞毒性与其分子中双键存在与否有着密切关系 .当甾核或支链中双键被饱和时 ,其细胞毒性均明显降低 .甾醇(5 )和 (8)对胃癌 (MGC)、宫颈癌 (HEL A)细胞的生长具有一定的抑制作用 .

In this paper, we have prepared six analogues of 24-methylenecholest-4-en-3β,6β-diol(1) and investigated the relationships between the biological activity and their structures. The results showed that the double bond in the molecule played an impor tant role to the cytotoxicity of these polyhydroxysterols. Their cytotoxicity reduced obviously while the double bond in steroidal nucleus or side-chain was saturated. Compounds 5 and 8 showed a moderate cytotoxic activity against human gastric carcinoma cells(MGC) and cervical carcinoma cells(HELA).