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

被引：10

作者：

Szabon-Watola, Monika I. ^{[2
]}

Ulatowski, Sarah V. ^{[1
]}

George, Kathleen M. ^{[1
]}

Hayes, Christina D. ^{[1
]}

Steiger, Scott A. ^{[1
]}

Natale, Nicholas R. ^{[1
,2
]}

机构：

[1] Univ Montana, NIH COBRE Ctr Struct & Funct Neurosci, Missoula, MT 59812 USA

[2] Univ Idaho, Dept Chem, Moscow, ID 83843 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2014年 / 24卷 / 01期

基金：

美国国家科学基金会;

关键词：

Multidrug resistance transporter; Isoxazole; Dihydropyridine; Homology model; MULTIDRUG-RESISTANCE MODIFIERS; P-GLYCOPROTEIN; DRUG TRANSPORTER; 4-ISOXAZOLYL-1,4-DIHYDROPYRIDINES; DERIVATIVES; MODULATORS; DOCKING; UTILITY; DESIGN;

D O I：

10.1016/j.bmcl.2013.11.068

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (C) 2013 Elsevier Ltd. All rights reserved.

引用

页码：117 / 121

页数：5

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