应用化学2013,Vol.30Issue(6):628-632,5.DOI:10.3724/SP.J.1095.2013.20352
3-取代-12-氧代-N,N-双(2-氯乙基)脱氧胆酰胺的合成及其抑制癌细胞活性
Synthesis and Antiproliferative Activity of 3-Substituted-12-oxy-N, N-bis (2-chloroethyl)-7-deoxycholic Amides
摘要
Abstract
Using 7-deoxycholic acid (1) as a starting material,3,12-dioxy-7-deoxycholic acid (2) was obtained by oxidation with Jones reagent.Then the N,N-bis(2-chloroethyl)-3,12-dioxy-7-deoxycholic amide (4) was synthesized by the reaction of compound 2 with bis (2-chloroethyl) amine.Furthermore,N,N-bis (2-chloroethyl)-12-oxy-3-hydroximino-7-deoxycholic amide (5) and N,N-bis (2-chloroethyl)-12-oxy-3-thiosemicarbazone-7-deoxycholic amide(6) were prepared by the functional group transformation of 3-carbonyl on compound 4.The antiproliferative activities of compounds against HeLa cells were assayed and the result showed that the compounds displayed distinct cytotoxicity.关键词
脱氧胆酸/氮芥/合成/抗肿瘤活性Key words
deoxycholic acid/ substituted-oxy-N/N-bis (chloroethyl)-deoxycholic amides /synthesis/ cytotoxicity分类
化学化工引用本文复制引用
甘春芳,苏绍烊,黄燕敏,林啟福,崔建国..3-取代-12-氧代-N,N-双(2-氯乙基)脱氧胆酰胺的合成及其抑制癌细胞活性[J].应用化学,2013,30(6):628-632,5.基金项目
广西自然科学基金(2010GXNSFD013019)和广西教育厅自然科学基金(201202ZD059)资助项目 (2010GXNSFD013019)