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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Synthesis and Antitumor Activity of Scopoletin Derivatives

Author(s): Jinpei Zhou, Lei Wang, Lijuan Wei, Yu Zheng, Huibin Zhang, Yubin Wang, Peng Cao, Ao Niu, Jing Wang, Yue Dai

Volume 9, Issue 4, 2012

Page: [397 - 401] Pages: 5

DOI: 10.2174/157018012799859972

Price: $65


Studies have shown that natural product scopoletin has significant pharmacological activities, such as antiarthritic, spasmolytic, antitumoral, antidepressant-like, antifungal, antihyperglycemic and antioxidative. In search of new antitumor agents, twelve scopoletin derivatives were designed and synthesized by a systematic combinatorial chemical approach and their chemical structures were confirmed by MS, IR, 1H NMR spectra and elemental analysis. Preliminary screening against mammary cells HUVEC and MCF-7 indicated that three compounds (5a, 5b, 5e) displayed reasonable antitumor activity with IC50 values below 18 μM whereas scopoletin showed its IC50 values above 100 μM. These results clearly indicated that structural modification of scopoletin can greatly increase its antitumor activity in vitro.

Keywords: Scopoletin, Synthesis, Cytotoxicity, Antitumour activity

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