| 引用本文: | 刘文虎,刘毅,常晋霞.2-(芳基哌嗪)乙酰氨基-5-取代-苯并噻唑衍生物的合成及抗肿瘤活性[J].中国现代应用药学,2014,31(3):278-283. |
| LIU Wenhu,LIU Yi,CHANG Jinxia.Synthesis and Antitumor Activity of 2-(Arylpiperazine) Acetamino-5-Substituted-Benzothiazole Compounds[J].Chin J Mod Appl Pharm(中国现代应用药学),2014,31(3):278-283. |
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| 摘要: |
| 目的 合成新型苯并噻唑衍生物并研究其抗肿瘤活性。方法 以3-取代苯胺为原料合成系列2-(芳基哌嗪)乙酰氨基-5-取代-苯并噻唑衍生物，采用MTT法测试了化合物对肿瘤细胞的抑制作用。结果 合成了12个新的苯并噻唑衍生物，化合物结构经1H-NMR、ESI-MS和元素分析确证。结论 多数目标化合物对5种肿瘤细胞株具抗增殖作用，部分化合物显示出与阳性对照药物5-氟尿嘧啶相当的抗肿瘤活性。 |
| 关键词: 苯并噻唑 合成 抗肿瘤活性 |
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| 基金项目:川北医学院重点发展项目(CBY11-A-ZP07)；南充市科技计划项目(13A0033) |
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| Synthesis and Antitumor Activity of 2-(Arylpiperazine) Acetamino-5-Substituted-Benzothiazole Compounds |
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LIU Wenhu1, LIU Yi1, CHANG Jinxia2
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1.Department of Pharmacology, North Sichuan Medical College, Nanchong 637007, China;2.Department of Microbiology and Immunology, North Sichuan Medical College, Nanchong 637007, China
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| Abstract: |
| OBJECTIVE To synthesize novel benzothiazole derivatives and investigate their antitumor activities. METHODS A series of 2-(arylpiperazine) acetamino-5-substituted-benzothiazole compounds were synthesized from 3-substituted anilines, and their antitumor activities were evaluated in vitro by the standard MTT assay. RESULTS Twelve novel benzothiazole derivatives were synthesized and their structures were confirmed with 1H-NMR, ESI-MS and elemental analysis. CONCLUSION Most of the target compounds showed antitumor activities against the tested tumor cells, and some compounds were comparable with that of 5-FU. |
| Key words: benzothiazoles synthesis antitumor activity |
