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.

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► 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.