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.