17α-[4,4-difluoro-8-(4-ethynylphenyl)-1,3,5,7-tetramethyl-4-bora-3a,4a-diaza-s-indacene]-7α-methyltestosterone

17α-[4,4-difluoro-8-(4-ethynylphenyl)-1,3,5,7-tetramethyl-4-bora-3a,4a-diaza-s-indacene]-7α-methyltestosterone is a steroid-fluorophore conjugate designed as a theranostic agent for the targeted imaging and treatment of androgen receptor (AR)-positive cancers. The molecule consists of a 7α-methyltestosterone (mibolerone) scaffold, which serves as a high-affinity ligand for the androgen receptor, covalently linked at the 17α position to a BODIPY (boron-dipyrromethene) fluorophore via an ethynylphenyl spacer. This conjugation enables the selective internalization of the dye into AR-expressing cancer cells, such as specific prostate and breast cancer lines, through receptor-mediated endocytosis. Beyond its utility as a fluorescent probe for cellular imaging, the BODIPY moiety acts as a photosensitizer; upon irradiation with visible light, it generates reactive oxygen species (ROS) that induce localized cytotoxicity. This dual functionality allows the compound to serve both as a diagnostic tool for visualizing tumor cells and as a therapeutic agent for photodynamic therapy (PDT).

Other names

7α-methyltestosterone-BODIPY conjugateMibolerone-BODIPY conjugate7α-Me-testosterone-BODIPY