期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 105, 期 -, 页码 145-155出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2015.09.013
关键词
JMJD2A inhibitors; 5-Carboxy-8-hydroxyquinoline; Anti-tumor; Physicochemical properties
资金
- National Natural Science Foundation of China [81230078, 81202463, 81502915, 81173087, 91129732]
- National Major Science and Technology Project of China [2014ZX09507002-005-015, 2013ZX09402102-001-005, 2010ZX09401-401]
- Priority Academic Program Development of Jiangsu Higher Education Institutions
A series of JMJD2A inhibitors had been designed by analyzing the binding mode of 5-carboxy-8-hydroxyquinoline (5-carboxy-8-HQ) with JMJD2A. The inhibitory activity of the synthesized compounds against JMJD2A was determined, followed by docking simulations to understand the structure activity relationships. Compounds with potent JMJD2A inhibitory activity demonstrated outstanding selectivity for JMJD2A over PHD2. Several potent compounds were selected to evaluate their anti-proliferative activity on tumor cell lines. Among them, compound 6p displayed the best anti-proliferative activity. Based on these in vitro biological data, seven compounds were chosen to determine their physicochemical properties. Compound 6p displayed good aqueous solubility and better permeability than 5-carboxy-8-HQ Our data recognized that compound 6p could be considered as a starting point for development of new Jmjc inhibitors. (C) 2015 Elsevier Masson SAS. All rights reserved.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据