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多羟基甾醇的合成及其结构与抗肿瘤细胞活性关系研究
引用本文:崔建国,曾陇梅,苏镜娱,彭文烈,徐安龙. 多羟基甾醇的合成及其结构与抗肿瘤细胞活性关系研究[J]. 高等学校化学学报, 2000, 21(9): 1399
作者姓名:崔建国  曾陇梅  苏镜娱  彭文烈  徐安龙
作者单位:1. 中山大学化学与化学工程学院;2. 中山大学生命科学院, 广州 510275;3. 广西师范学院化学系, 南宁 530001
基金项目:中国科学院资助项目,广东省博士启动基金
摘    要: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(HELA)细胞的生长具有一定的抑制作用.

关 键 词:多羟基甾醇  甾醇合成  细胞毒性  构效关系  
收稿时间:1999-08-21

Synthesis of Some Polyhydroxysterols and Investigation of Relationship Between Their Structure and Cytotoxicity
CUI Jian-Guo,ZENG Long-Mei,SU Jing-Yu,PENG Wen-Lie,XU An-Long. Synthesis of Some Polyhydroxysterols and Investigation of Relationship Between Their Structure and Cytotoxicity[J]. Chemical Research In Chinese Universities, 2000, 21(9): 1399
Authors:CUI Jian-Guo  ZENG Long-Mei  SU Jing-Yu  PENG Wen-Lie  XU An-Long
Affiliation:1. Schoolof Chemistryand Chemical Engineering, Zhongshan University, Guangzhou 510275, China;2. Schoolof Life Science, Zhongshan University, Guangz hou 510275, China;3. Depa rtment of Chemistry, Guangx i Teachers College, Nanning 530001, China
Abstract: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).
Keywords:Polyhydroxysterols  Synthesis of sterols  Cytotoxicity  Structure activity relationship  
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