Synthesis and in vitro antitumor activity of novel scopoletin derivatives

Twenty scopoletin derivatives were developed by a systematic combinatorial chemical approach and their chemical structures were confirmed by MS, IR, 1H NMR spectra and elemental analysis. Primary screening against mammary (MCF-7 and MDA-MB 231) and colon (HT-29) carcinoma cells indicated that five compounds (8d, 8g, 8j, 11b and 11g) displayed high antitumor potencies with IC50 values below 20 μM whereas scopoletin showed IC50 values above 100 μM. Moreover, the most promising compound 11g was more active than 5-fluorouracil. These results clearly indicated that the modification of the scopoletin structure could greatly increase its antitumor activity in vitro.

Graphical abstractTwo series of scopoletin derivatives were synthesized and investigated for cytotoxicity against mammary (MCF-7, MDA-MB 231) and colon (HT-29) carcinoma cell lines.Figure optionsDownload full-size imageDownload as PowerPoint slide