Synthesis and in vitro antitumor activity of novel scopoletin derivatives
Copyright policy )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, (1)H 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 IC(50) values below 20 μM whereas scopoletin showed IC(50) 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.
- Freie Universität Berlin Germany
- China Pharmaceutical University China (People's Republic of)
- University of Innsbruck Austria
Scopoletin, Structure-Activity Relationship, Cell Line, Tumor, Humans, Antineoplastic Agents, Apoptosis, Cell Cycle Checkpoints, Drug Screening Assays, Antitumor
Scopoletin, Structure-Activity Relationship, Cell Line, Tumor, Humans, Antineoplastic Agents, Apoptosis, Cell Cycle Checkpoints, Drug Screening Assays, Antitumor
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