• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验

Synthesis and biological evaluation of (hetero)arylmethyloxy- and arylmethylamine-phenyl derivatives as potent P-glycoprotein modulating agents.

作者信息

Colabufo Nicola Antonio, Berardi Francesco, Perrone Roberto, Rapposelli Simona, Digiacomo Maria, Vanni Michael, Balsamo Aldo

机构信息

Dipartimento farmacochimico, Universita degli Studi di Bari, Bari, Italy.

出版信息

J Med Chem. 2008 Mar 13;51(5):1415-22. doi: 10.1021/jm701267q. Epub 2008 Feb 8.

DOI:10.1021/jm701267q
PMID:18257545
Abstract

Starting from lead compounds 12b and 28b, previously characterized as P-glycoprotein (P-gp) modulating agents, two series of new compounds were investigated. Compounds 14a, b and 15a, b displayed high P-gp modulating activity in the submicromolar range (EC 50 values from 0.25 to 0.80 microM). Moreover, amino derivatives 23- 27 showed EC 50 values ranging from 0.085 to 0.90 microM. In the pyridyl series, the best result has been obtained for 4-pyridyl derivative 17b (EC 50 = 0.85 microM). The best P-gp modulating agents 14a, b, 15a, b, and 23- 27 also have been studied for determining their breast cancer resistance protein (BCRP) inhibition activity. The results demonstrated that only the amino derivatives 23- 27 displayed moderate BCRP inhibition activity.

摘要

相似文献

1
Synthesis and biological evaluation of (hetero)arylmethyloxy- and arylmethylamine-phenyl derivatives as potent P-glycoprotein modulating agents.
J Med Chem. 2008 Mar 13;51(5):1415-22. doi: 10.1021/jm701267q. Epub 2008 Feb 8.
2
Flavonoids inhibit breast cancer resistance protein-mediated drug resistance: transporter specificity and structure-activity relationship.黄酮类化合物抑制乳腺癌耐药蛋白介导的耐药性：转运体特异性及构效关系
Cancer Chemother Pharmacol. 2007 Nov;60(6):789-97. doi: 10.1007/s00280-007-0426-7. Epub 2007 Mar 8.
3
Reversal of P-gp and BCRP-mediated MDR by tariquidar derivatives.他立喹达衍生物对P-糖蛋白和乳腺癌耐药蛋白介导的多药耐药的逆转作用。
Eur J Med Chem. 2015 Aug 28;101:560-72. doi: 10.1016/j.ejmech.2015.06.049. Epub 2015 Jul 10.
4
Characterization of efflux transporters involved in distribution and disposition of apixaban.鉴定与阿哌沙班分布和处置相关的外排转运体。
Drug Metab Dispos. 2013 Apr;41(4):827-35. doi: 10.1124/dmd.112.050260. Epub 2013 Feb 4.
5
Discovery of alkoxyl biphenyl derivatives bearing dibenzo[c,e]azepine scaffold as potential dual inhibitors of P-glycoprotein and breast cancer resistance protein.发现具有二苯并[c,e]氮杂䓬骨架的烷氧基联苯衍生物作为P-糖蛋白和乳腺癌耐药蛋白的潜在双重抑制剂。
Bioorg Med Chem Lett. 2014 Aug 1;24(15):3419-21. doi: 10.1016/j.bmcl.2014.05.081. Epub 2014 Jun 4.
6
Amine linked flavonoid dimers as modulators for P-glycoprotein-based multidrug resistance: structure-activity relationship and mechanism of modulation.胺键连接的黄酮类二聚体作为基于 P-糖蛋白的多药耐药性调节剂：结构-活性关系和调节机制。
J Med Chem. 2012 Mar 8;55(5):1999-2014. doi: 10.1021/jm201121b. Epub 2012 Feb 22.
7
Parguerenes: Marine red alga bromoditerpenes as inhibitors of P-glycoprotein (ABCB1) in multidrug resistant human cancer cells.派格来恩：海洋红藻溴二萜作为多药耐药性人类癌细胞中 P 糖蛋白（ABCB1）的抑制剂。
Biochem Pharmacol. 2013 May 1;85(9):1257-68. doi: 10.1016/j.bcp.2013.02.005. Epub 2013 Feb 13.
8
HM30181 Derivatives as Novel Potent and Selective Inhibitors of the Breast Cancer Resistance Protein (BCRP/ABCG2).HM30181衍生物作为乳腺癌耐药蛋白（BCRP/ABCG2）新型强效选择性抑制剂
J Med Chem. 2015 May 14;58(9):3910-21. doi: 10.1021/acs.jmedchem.5b00188. Epub 2015 Apr 24.
9
Arylamino Esters As P-Glycoprotein Modulators: SAR Studies to Establish Requirements for Potency and Selectivity.芳氨基酯作为P-糖蛋白调节剂：建立效力和选择性要求的构效关系研究
ChemMedChem. 2015 Aug;10(8):1339-43. doi: 10.1002/cmdc.201500143. Epub 2015 May 26.
10
Multi-drug-resistance-reverting agents: 2-aryloxazole and 2-arylthiazole derivatives as potent BCRP or MRP1 inhibitors.多药耐药逆转剂：作为有效的乳腺癌耐药蛋白（BCRP）或多药耐药相关蛋白1（MRP1）抑制剂的2-芳基恶唑和2-芳基噻唑衍生物
ChemMedChem. 2009 Feb;4(2):188-95. doi: 10.1002/cmdc.200800329.

引用本文的文献

1
Iodine(III)-Mediated Oxidation of Anilines to Construct Dibenzazepines.碘(III)介导的苯胺氧化构建二苯并氮杂卓。
Chemistry. 2023 Jul 3;29(37):e202301141. doi: 10.1002/chem.202301141. Epub 2023 May 11.
2
Investigating Curcumin/Intestinal Epithelium Interaction in a Millifluidic Bioreactor.在微流控生物反应器中研究姜黄素与肠上皮的相互作用
Bioengineering (Basel). 2020 Aug 26;7(3):100. doi: 10.3390/bioengineering7030100.
3
Models used to screen for the treatment of multidrug resistant cancer facilitated by transporter-based efflux.
用于筛选基于转运体外排作用的多药耐药癌症治疗方法的模型。
J Cancer Res Clin Oncol. 2019 Aug;145(8):1949-1976. doi: 10.1007/s00432-019-02973-5. Epub 2019 Jul 10.
4
Synthesis and In Vivo Imaging of N-(3-[C]Methoxybenzyl)-2-(3-Methoxyphenyl)ethylaniline as a Potential Targeting Agent for P-glycoprotein.N-（3-[碳-11]甲氧基苄基）-2-（3-甲氧基苯基）乙胺作为P-糖蛋白潜在靶向剂的合成与体内成像
Mol Imaging Biol. 2016 Dec;18(6):916-923. doi: 10.1007/s11307-016-0965-6.
5
Subtle Structural Differences Trigger Inhibitory Activity of Propafenone Analogues at the Two Polyspecific ABC Transporters: P-Glycoprotein (P-gp) and Breast Cancer Resistance Protein (BCRP).细微的结构差异引发普罗帕酮类似物对两种多特异性ABC转运蛋白的抑制活性：P-糖蛋白（P-gp）和乳腺癌耐药蛋白（BCRP）。
ChemMedChem. 2016 Jun 20;11(12):1380-94. doi: 10.1002/cmdc.201500592. Epub 2016 Mar 10.
6
Development of classification models for identifying "true" P-glycoprotein (P-gp) inhibitors through inhibition, ATPase activation and monolayer efflux assays.通过抑制、ATP酶激活和单层外排试验开发用于鉴定“真正”P-糖蛋白（P-gp）抑制剂的分类模型。
Int J Mol Sci. 2012;13(6):6924-6943. doi: 10.3390/ijms13066924. Epub 2012 Jun 7.
7
A novel approach for predicting P-glycoprotein (ABCB1) inhibition using molecular interaction fields.一种使用分子相互作用场预测 P 糖蛋白（ABCB1）抑制作用的新方法。
J Med Chem. 2011 Mar 24;54(6):1740-51. doi: 10.1021/jm101421d. Epub 2011 Feb 22.