3-(四氮唑-5-基)-2-亚胺香豆素衍生物:合成、表征和肿瘤细胞系评价

A. Bouattour, M. Fakhfakh, Souhir Abid El-Gharbi, M. Abid, L. Paquin, R. Guével, T. Charlier, H. Ammar, J. Bazureau
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引用次数: 1

摘要

本文首次报道了新的3-(四氮唑-5-基)-2-亚氨基香豆素衍生物。该化合物分两步制备,收率为55 ~ 93%。通过1H、13C NMR、FTIR、UV-Visible和HRMS对其进行了表征。对6种具有代表性的人肿瘤细胞系(Huh 7-D12、Caco2、MDA-MB231、HCT 116、PC3和NCI-H727)和HaCat角质形成细胞进行了抗增殖活性测试。其中化合物5e对HCT 116有活性(IC50为15 μM)。
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3-(Tetrazol-5-yl)-2-imino-coumarins Derivatives: Synthesis, Characterization, and Evaluation on Tumor Cell Lines
The first report of new 3-(tetrazol-5-yl)-2-iminocoumarin derivatives is described. The title compounds were prepared in two steps and were obtained in good yields (55-93%). They have been fully characterized by 1H, 13C NMR, FTIR, UV-Visible and HRMS. They were tested for their antiproliferative activities against six representative human tumor cell lines (Huh 7-D12, Caco2, MDA-MB231, HCT 116, PC3 and NCI-H727) and HaCat keratinocytes. Among them, compound 5e was active on HCT 116 (IC50 15 μM).
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