Efficient synthesis and antiproliferative activity of novel thioether-substituted flavonoids

• A microwave-assisted synthesis of thioether-substituted flavonoids was developed.
• 57 novel flavonoids were synthesized and screened against six tumor cell lines.
• Three candidates with promising antitumor activity were successfully identified.

As widely occurring natural products, flavonoids are an important source for drug discovery, due to their structural diversity and broad-spectrum biological activity. In this work, a library of novel, thioether-substituted flavonoids with diverse heterocyclic groups was synthesized via a microwave-assisted procedure with the advantages of good yields, short times, mild conditions and ready isolation of the products. Their antiproliferative activities were evaluated against six cancer cell lines, HCCLM-7, Hela, MDA-MB-435S, SW-480, Hep-2, and MCF-7 by the MTT-based assay. Compared with the positive control 5-fluorouracil, three compounds, 6a, 6b and 6j were successfully identified as the most promising candidates, due to their higher potency and broad-spectrum bioactivity with IC50 values in the range of 0.43 μM–6.7 μM.

A library of 57 novel flavonoids bearing diverse heterocyclic groups was efficiently synthesized via microwave-assisted procedure. Three candidates with promising potent and broad-spectrum antitumor activity were successfully identified.Figure optionsDownload as PowerPoint slide