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| 20(S)-O-取代苯甲酸-7-乙基喜树碱酯类化合物的合成及其抗肿瘤活性 | |
| 引用本文： | 高鹏,朱磊,王佳乐,王浦海,孙立,袁胜涛.20(S)-O-取代苯甲酸-7-乙基喜树碱酯类化合物的合成及其抗肿瘤活性[J].合成化学,2012,20(2):137-142. |
| 作者姓名： | 高鹏 朱磊 王佳乐 王浦海 孙立 袁胜涛 |
| 作者单位： | 1. 南京工业大学药学院,江苏南京,211816 2. 南京工业大学江苏省药物研究所,江苏南京,211816 3. 中国药科大学国家南京新药筛选中心,江苏南京,211009 |
| 基金项目： | 国家自然科学基金资助项目 |
| 摘 要： | 在AcOH/98％ H2S04体系中,喜树碱和正丙醛经烷基化反应制得7-乙基喜树碱(2)；以1-乙基-3-(3-二甲基氨基丙基)碳二亚胺盐酸盐为脱水剂,4-二甲氨基吡啶为催化剂,2与取代苯甲酸直接酯化合成了一系列新型的20(S)-O-取代苯甲酸-7-乙基喜树碱酯类化合物(4a -4k),其结构经1H NMR,IR和MS表征.采用MTT法初步考察了4a～4k对人肺癌细胞(LLC-E9FP),人肺腺癌细胞(95D),人胃癌细胞(BGC-803),人胃癌细胞( HGC-27)和人肝癌细胞(7721)的抑制活性.结果表明,4b和4e对LLC-E9FP具有明显强于喜树碱的抑制活性；4h～4k对HGC-27,95D,7721也有明显的抑制活性. |
| 关 键 词： | 喜树碱酯 取代苯甲酸 合成 抗肿瘤活性 |
Synthesis and Antitumor Activities of 20 (S)-O-linked Substituted Benzoic Acid-7-ethyl Camptothecin Ester Compounds |
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| GAO Peng , ZHU Lei , WANG Jia-le , WANG Pu-hai , SUN Li , YUAN Sheng-tao.Synthesis and Antitumor Activities of 20 (S)-O-linked Substituted Benzoic Acid-7-ethyl Camptothecin Ester Compounds[J].Chinese Journal of Synthetic Chemistry,2012,20(2):137-142. | |
| Authors: | GAO Peng ZHU Lei WANG Jia-le WANG Pu-hai SUN Li YUAN Sheng-tao |
| Institution: | 2(a.School of Pharmaceutical Sciences;b.Jiangsu Institute of Materia Medica, 1.Nanjing University of Technology,Nanjing 211816,China; 2.National Nanjing Center for Drug Screening,China Pharmaceutical University,Nanjing 211009,China) |
| Abstract: | 7-Ethyl camptothecin(2) was obtained by alkylation of camptothecin with propaldehyde in AcOH/98%H2SO4.Eleven novel 20(S)-O-linked substituted benzoic acid-7-ethyl camptothecin ester compounds(4a~4k) were synthesized by straightforward esterification of 2 with substituted-benzoic acid using 1-3-(3-dimethylaminopropyl)-3-ethyl carbodiimide hydrochloride as the dehydrator and 4-dimethylamiopryidine as the catalyst.The structures were characterrized by 1H NMR,IR and MS.Antitumor activities of 4a~4k were investigated against five human cancer cell lines(LLC-E9FP,95D,BGC-803,HGC-27 and 7721) by MTT method in vitro.The results showed that 4b and 4e had significantly stronger antitumor activities against LLC-E9FP cell than that of camptothecin,and 4h~4k exhibited a certain antitumor activities against HGC-27,95D and 7721 cells. |
| Keywords: | camptothecin ester substituted benzoic acids synthesis antitumor activity |
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