Fluorescent probes of the isoxazole-dihydropyridine scaffold: MDR-1 binding and homology model.

ABSTRACT: Isoxazole-1,4-dihydropyridines (IDHPs) were tethered to fluorescent moieties using double activation via a lanthanide assisted Weinreb 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.

SUBMITTER: Szabon-Watola MI 

PROVIDER: S-EPMC3987963 | biostudies-literature | 2014 Jan

REPOSITORIES: biostudies-literature