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Literature DB >> 24342237

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

Monika I Szabon-Watola¹, Sarah V Ulatowski², Kathleen M George², Christina D Hayes², Scott A Steiger², Nicholas R Natale³.

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.

Entities: CellLine Chemical Disease Gene Species

Keywords: Dihydropyridine; Homology model; Isoxazole; Multidrug resistance transporter

Mesh：

Substances：

Year: 2013 PMID： 24342237 PMCID： PMC3987963 DOI： 10.1016/j.bmcl.2013.11.068

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

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