Design, synthesis and antiproliferative activity of scopoletin derivatives

HU Jinglin; LI Linhu; CHEN Li

doi:10.11665/j.issn.1000-5048.20150205

Journal of China Pharmaceutical University > 2015 > 46(2): 169-173. > DOI: 10.11665/j.issn.1000-5048.20150205

HU Jinglin, LI Linhu, CHEN Li. Design, synthesis and antiproliferative activity of scopoletin derivatives[J]. Journal of China Pharmaceutical University, 2015, 46(2): 169-173. DOI: 10.11665/j.issn.1000-5048.20150205

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Design, synthesis and antiproliferative activity of scopoletin derivatives

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To explore novel scopoletin derivatives with more potent antiproliferative activity, a series of compounds were designed and synthesized( 10a - 10i )by linking benzamide to scopoletin′s framework. Their structures were determined by ESI-MS, IR and ¹H NMR. The antiproliferative activity of the synthetic derivatives against human cancer cells MCF-7, A549 and HCT-116 was evaluated by MTT assay. Preliminary experimental results showed that compound 10g was the most potent one, whose antiproliferative activity was stronger than that of the positive control scopoletin and sunitinib.
- scopoletin,
- derivative,
- synthesis,
- antiproliferative activity

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