Convenient synthesis of novel geiparvarin analogs with potential anti-cancer activity via click chemistry

Based on the advantages of natural products in new anti-cancer drug development, we synthesized a series of novel benzopyran-4-one derivatives and evaluated their in vitro anti-cancer activities. The bioassays showed that the majority of the resultant compounds exerted anti-tumor effect against six human cancer cell lines to various extents, which supported the rationale of the design. Compound 5s exhibited highest potency of all the synthesized compounds.

This work describes the design and synthesis of geiparvarin analogs with moderate to good in vitro anti-cancer activity and the compound 5s was the most potential one.Figure optionsDownload as PowerPoint slideHighlights
► We design and synthesized 20 novel geiparvarin analogs.
► Bioisosteric transformation method was employed for the drug design strategy.
► We determine the cycloaddition was trans-addition via X-ray crystallography.
► 21 compounds were evaluated for their in vitro cytotoxic activities.
►  The results showed some of resultant compounds have potential anti-cancer activity.