Synthesis and biological evaluation of novel ferrocenyl curcuminoid derivatives

Anusch Arezki (1) , Guy G. Chabot (2) , Lionel Quentin (2) , Daniel Scherman (1, 2) , Gérard Jaouen (1) , Emilie Brulé (1)

1 Laboratoire Charles Friedel
2 UPCGI - UMR 8151 / UMR_S 1022 - Unité de pharmacologie chimique et génétique et d'imagerie

With the purpose to improve the biological activities of curcumin, eight novel ferrocenyl curcuminoids were synthesized by covalent anchorage of three different ferrocenyl ligands. We evaluated their cytotoxicity on B16 melanoma cells and normal NIH 3T3 cells, their inhibition of tubulin polymerization and their effect on the morphology of endothelial cells. The presence of a ferrocenyl side chain was clearly shown to improve the biological activity of most of their corresponding organic curcuminoid analogues.

Keywords: curcuminoid; ferrocenyl; B16 melanoma; NIH 3T3 cells; endothelial cells; cancer

Domains: Cancer

Anusch Arezki, Guy G. Chabot, Lionel Quentin, Daniel Scherman, Gérard Jaouen, et al.. Synthesis and biological evaluation of novel ferrocenyl curcuminoid derivatives. MedChemComm, 2011, 2 (3), pp.190-195. ⟨10.1039/c0md00231c⟩. ⟨inserm-00709892⟩