喜树碱氨基酸衍生物的合成及细胞毒活性研究  

Synthesis and Cytotoxic Activity of Camptothecin Amino Acid Derivatives

作　　者：马玉冰 康威 李朝阳 龚显峰[1] 张华[1] Ma Yubing;Kang Wei;Li Chaoyang;Gong Xianfeng;Zhang Hua(Department of Pharmaceutical Engineering,Heilongjiang University,Harbin 150080,China;The High School Attached to Harbin Institue of Technology,Harbin 150083,China;Sinopharm Yixin Pharmaceutical Co.,Ltd.,Changhuan 130012,China)

机构地区：[1]黑龙江大学制药工程系,黑龙江哈尔滨150080 [2]哈尔滨工业大学附属中学,黑龙江哈尔滨150083 [3]国药一心制药有限公司,吉林长春130012

出　　处：《山东化工》2020年第6期52-55,共4页Shandong Chemical Industry

摘　　要：喜树碱与丁二酸酐酯化得到中间体20(S)-O-4-氧代戊酸酰基喜树碱3a,再与L-氨基酸酯盐酸盐缩合得到10个喜树碱氨基酸酯衍生物4a^4j。目标化合物经过IR、1H-NMR、13 C-NMR、MS、元素分析等结构确证。采用四甲基偶氮唑盐法考察了目标化合物对人肝癌细胞、人结肠癌细胞体外抑制活性。结果表明化合物4b,4d,4e,4i,4j抑制率较高。We use commercial camptothecin as the starting material to obtain intermediate 20(S)-O-4-oxopentanoic acid acyl camptothecin 3a by catalytic esterification.The intermediates were condensed with L-amino acid ester hydrochloride respectively to obtain camptothecin amino acid derivatives 4a-4j.The structure of the compounds was confirmed by IR,1H-NMR,13 C-NMR,MS,elemental analysis.The in vitro activity test of the compounds against Human hepatoma cells and Human colon cancer cells was examined by MTT assay.The results showed that the compounds 4b,4d,4e,4i,4j had higher inhibitory activity in vitro.

关 键 词：喜树碱氨基酸衍生物 合成 四甲基偶氮唑盐法 

分 类 号：R914[医药卫生—药物化学]