Fluorophore-tagged pharmacophores for antitumor cytotoxicity: Modified chiral lipidic dialkynylcarbinols for cell imaging - Archive ouverte HAL Accéder directement au contenu
Article Dans Une Revue Bioorganic and Medicinal Chemistry Letters Année : 2015

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.
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Dates et versions

hal-01915503 , version 1 (07-11-2018)

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Dymytrii Listunov, S. Mazeres, Yulian Volovenko, Etienne Joly, Yves Génisson, et al.. Fluorophore-tagged pharmacophores for antitumor cytotoxicity: Modified chiral lipidic dialkynylcarbinols for cell imaging. Bioorganic and Medicinal Chemistry Letters, 2015, 25 (20), pp.4652-4656. ⟨10.1016/j.bmcl.2015.08.029⟩. ⟨hal-01915503⟩
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