Thieno[2,3-b]pyridines-A new class of multidrug resistance (MDR) modulators

被引：37

作者：

Krauze, Aivars ^{[1
]}

Grinberga, Signe ^{[1
]}

Krasnova, Laura ^{[1
]}

Adlere, Ilze ^{[1
]}

Sokolova, Elina ^{[1
]}

Domracheva, Ilona ^{[1
]}

Shestakova, Irina ^{[1
]}

Andzans, Zigmars ^{[1
]}

Duburs, Gunars ^{[1
]}

机构：

[1] Latvian Inst Organ Synth, LV-1006 Riga, Latvia

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2014年 / 22卷 / 21期

关键词：

Thieno[2,3-b]pyridine; Multidrug resistance modulators; P-glycoprotein; Multidrug resistance-associated protein; Breast cancer resistance protein; P-GLYCOPROTEIN; DERIVATIVES; INHIBITORS; THIENOPYRIDINE; AGENTS; REVERSAL; PROTEIN; DESIGN; BCRP; ABC;

D O I：

10.1016/j.bmc.2014.09.023

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

To identify new potent multidrug resistance modulators, we have synthesized a series of novel thieno[ 2,3-b]pyridines and furo[2,3-b] pyridines, and examined their stucture-activity relationships. All synthesized compounds were tested to determine BCRP1, P-gp, and MRP1 inhibitor activity, and most potent MDR modulators were also screened for their toxicity, cytotoxicity and Ca2+ channel antagonist activity. Among these compounds, thieno[2,3-b] pyridine (6r) was found to exhibit a potent P-gp inhibitory action with EC50 = 0.3 +/- 0.2 mu M, MRP1 inhibitory action with EC50 = 1.1 +/- 0.1 mu M and BCRP1 inhibitory action with EC50 = 0.2 +/- 0.05 mu M and may represent suitable candidate for further pharmacological studies. (C) 2014 Elsevier Ltd. All rights reserved.

引用

页码：5860 / 5870

页数：11

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