Synthesis of novel 2, 5-dihydrofuran derivatives and evaluation of their anticancer activity

According to metal-catalyzed [3 + 2] cycloaddition reaction, we synthesized a series of novel 2, 5-dihydrofuran derivatives and evaluated their in vitro anti-cancer activities via MTT method. The bioassay showed that the majority of the resultant compounds exerted anti-tumor effect against four human cancer cell lines to various extents, which supported the rationale of the design. Compounds 9e and 10g showed the highest activity with broad anti-cancer spectrum, which were good candidates for further evaluation.

Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slideHighlights► We synthesized a series of novel 2, 5-dihydrofuran derivatives. ► Metal-catalyzed [3 + 2] cycloaddition reaction was employed. ► We determine the reaction mediate via X-ray crystallography. ► All resultant compounds were evaluated for their in vitro cytotoxic activities. ► The result shows some of resultant compounds have potential anti-cancer activity.