咨询与建议

看过本文的还看了

相关文献

该作者的其他文献

文献详情 >Synthesis of reversible PAD4 i... 收藏

Synthesis of reversible PAD4 inhibitors via copper-catalyzed C-H arylation of benzimidazole

Synthesis of reversible PAD4 inhibitors via copper-catalyzed C-H arylation of benzimidazole

作     者:Zhengwei Guo Lai Shi Bo Wang Gang He Yanming Wang Gong Chen 

作者机构:State Key Laboratory and Institute of Elemento-Organic ChemistryCollege of ChemistryNankai University School of Life SciencesHenan University Department of Biochemistry and Molecular BiologyThe Pennsylvania State University 

出 版 物:《Science China Chemistry》 (中国科学(化学英文版))

年 卷 期:2019年第62卷第5期

页      面:592-596页

核心收录:

学科分类:1007[医学-药学(可授医学、理学学位)] 10[医学] 

基  金:supported by the National Natural Science Foundation of China(21502098,21672105,21725204,91753124) Natural Science Foundation of Tianjin(17JCYBJC19700,18JCZDJC32800) Qingdao National Laboratory for Marine Science and Technology the State Key Laboratory of Elemento-Organic Chemistry at Nankai University 

主  题:C–H arylation benzimidazoles PAD4 inhibitor copper catalysis 

摘      要:PAD4 is a promising epigenetic drug target for various cancers and immune diseases. In this work, we applied a Cu-catalyzed C–H arylation reaction of N-heteroarene to the synthesis of complex non-covalent PAD4 inhibitors bearing a bi-heteroaryl pharmacophore. This strategy allowed us to access various analogs of C_2-aryl substituted benzimidazoles from a common benzimidazole core and easily accessible aryl iodides. Preliminary SAR studies revealed the indole motif of GSK-484 is critical to its activity. Replacing the N-cyclopropylmethyl group to N-benzyl group on the indole ring of GSK-484 resulted in more than5-fold increase in cell killing efficacy against 4T1 cell line.

读者评论 与其他读者分享你的观点

用户名:未登录
我的评分