Fluorophore-tagged pharmacophores for antitumor cytotoxicity: Modified chiral lipidic dialkynylcarbinols for cell imaging
Résumé
Chiral lipidic dialkynylcarbinols (DACs), recently highlighted as antitumoral pharmacophores, have been conjugated to difluoroboron-dipyrromethene (bodipy), 7-hydroxycoumarin, and 7-nitrobenzoxadiazole (NBD) fluorophore motifs through triazole clips. The labeled lipids preserve cytotoxic activity against HCT116 cells, and fluorescence microscopy of the stained cells showed clear signals in the intracellular membrane system. While the bodipy conjugate also labels lipid droplets very brightly, as expected, the coumarin and NBD probes appear as promising specific tools for the identification of the intracellular targets of DACs' cytotoxicity.