Isoxazole-1,4-Dihydropyridines (IDHPs) were tethered to Fluorescent moieties using double activation via a lanthanide assisted Weibreb amidation. IDHP-fluorophore conjugate 3c exhibits the highest binding to date for IDHPs at the multidrug-resistance transporter (MDR-1), and IDHP-fluorophore conjugates 3c and 7 distribute selectively in SH-SY5Y cells. A homology model for IDHP binding at MDR-1 is presented which represents our current working hypothesis.
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