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新型双酰胺衍生物的合成及抗癌活性
引用本文:郑玉国.新型双酰胺衍生物的合成及抗癌活性[J].精细化工,2012,29(3):285-289,307.
作者姓名:郑玉国
作者单位:1. 贵州大学精细化工研究开发中心教育部绿色农药与农业生物工程重点实验室,贵州贵阳550025;兴义民族师范学院化学生物系,贵州兴义562400
2. 贵州大学精细化工研究开发中心教育部绿色农药与农业生物工程重点实验室,贵州贵阳,550025
3. 兴义民族师范学院化学生物系,贵州兴义,562400
基金项目:国家自然科学基金项目(面上项目,重点项目,重大项目)
摘    要:以取代苯甲酸为起始原料,设计合成了10个含苯并噻唑基双酰胺类化合物,其结构经1HNMR、13CNMR、IR及元素分析确证。采用MTT法进行化合物抑制PC3、BGC-823癌细胞体外活性测试,结果表明,所合成的化合物具有不同程度地抑制癌细胞活性,其中化合物N-2-(6-甲基苯并噻唑-2-氨基甲酰基)-4-甲基苯基]-4-氯苯甲酰胺(Ⅳa)和N-2-(4-甲基苯并噻唑-2-氨基甲酰基)-4-甲基苯基]-2-甲基苯甲酰胺(Ⅳe)在10μmol/L浓度下对PC3的抑制率为70.8%和68.4%,N-2-(苯并噻唑-2-氨基甲酰基)-4-甲基苯基]-2-甲基苯甲酰胺(Ⅳd)在10μmol/L浓度下对BGC-823的抑制率为65.9%。

关 键 词:双酰胺  苯并噻唑  抗癌活性  医药与日化原料
收稿时间:2011/11/6 0:00:00
修稿时间:2011/12/6 0:00:00

Synthesis and Antitumor Activity of Novel Bisamides Compounds
ZHENG Yu-guo.Synthesis and Antitumor Activity of Novel Bisamides Compounds[J].Fine Chemicals,2012,29(3):285-289,307.
Authors:ZHENG Yu-guo
Affiliation:1(1.Key Laboratory of Green Pesticide and Bioengineering,Ministry of Educational Research and Development Center for Fine Chemicals,Guizhou University,Guiyang 550025,Guizhou,China;2.Department of Chemistry and Biology,Xingyi Normal College,Xingyi 562400,Guizhou,China)
Abstract:Ten novel bisamide compounds containing benzothiazole unit were synthesized from the starting material of substituted benzoic acid.Their structures were characterized by means of 1HNMR,13CNMR,IR and elemental analyses.Preliminary bioassay indicates that some compounds posed antitumor activity to PC3 and BGC-823 cells in vitro by MTT method.The antiproliferation activity of compound N-2-(6-methylbenzothiazole-2-ylcarbamoyl)-4-methylphenyl]-4-chlorobenzenecarboxamide(Ⅳa) and N-2-(4-methylbenzothiazole-2-ylcarbamoyl)-4-methylphenyl]-2-methylbenzene carboxamide(Ⅳe) to PC3 cells at the concentration of 10 μmol/L was 70.8% and 68.4% respectively.And the antiproliferation activity of compound N-2-(benzothiazole-2-ylcarbamoyl)-4-methylphenyl]-2-methylbenzenecarboxamide(Ⅳd) to BGC-823 cells at the concentration of 10 μmol/L was 65.9%.
Keywords:bisamides  benzothiazol  Antitumor activity  
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