Synthesis and Antitumor Activity of Scopoletin Derivatives

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.