Solvent-free synthesis and in vitro cytotoxicity of fluorinated chalcones against HepG2 cells

A series of chalcones (1a-1g, 2a-2g, 3a-3g) containing fluoro substituents at various positions of both rings were synthesized via Claisen-Schmidt condensation using solvent-free grinding and microwave-assisted methods.Among synthesized chalcones, eleven structures (1f, 2b, 2d-2g, 3b-3d, 3f-3g) are novel compounds.Based on the fact that fluorinated organic compounds displayed promising anticancer activities, fluorinated chalcones were assayed for cytotoxicity against HepG2 cancer cells by determining their IC50 values.We found three structures (1c, IC50 = 63.386.76M; 1e, IC50 = 59.331.10M; 1g, IC50 = 43.186.54M) showing highest the antiproliferative activities.The in vitro results indicated the effects of the position of fluoro substituents on the cytotoxic activity.In particular, the scaffold of 4-F chalcone might be regarded as playing a crucial role in the promising anticancer inhibitory effects towards HepG2 cells.