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OALib Journal期刊
ISSN: 2333-9721
费用：99美元
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2-(3-丁炔酰胺基苯基)苯并噻唑衍生物的合成及抗肿瘤活性研究
, PP. 888-895
Keywords: 苯并噻唑,抗肿瘤活性,构效关系
Abstract:
以4-氟-3-硝基苯甲酸为起始原料，通过两条合成路线，经5～7步反应得到20个全新的2-（3-丁炔酰胺基苯基）苯并噻唑类化合物。目标化合物的结构经1hnmr和hr-ms鉴定。采用mtt法考察了其对5种肿瘤细胞株（hct116、mia-paca2、u87-mg、a549、nci-h1975）的抗增殖作用，结果表明大部分化合物选择性地对其中的3种肿瘤细胞具有明显的抗增殖活性，其中化合物14c对人脑胶质母细胞瘤u87-mg细胞、化合物14h对结肠癌hct116细胞的ic50值均在1×10-8mol·l-1数量级水平，在此基础上对该类化合物进行了初步构效分析。
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