Discovery and structure activity relationship study of novel indazole amide inhibitors for extracellular signal-regulated kinase1/2 (ERK1/2)

Autor:	Cao Jianhua, Lei Jiang, Xiao-Tong Yang, Chen Zhuxi, Liu Feifei, Shuai Tang, Min Huang, Nan Jin, Jian Ding, Meiyu Geng, Li Lei
Rok vydání:	2016
Předmět:	0301 basic medicine Models Molecular Indazoles Clinical Biochemistry Mutant Pharmaceutical Science Biochemistry 03 medical and health sciences HT29 Cells chemistry.chemical_compound Structure-Activity Relationship 0302 clinical medicine Amide Drug Discovery Extracellular Structure–activity relationship Humans neoplasms Molecular Biology Protein Kinase Inhibitors Mitogen-Activated Protein Kinase 1 Indazole Mitogen-Activated Protein Kinase 3 biology Dose-Response Relationship Drug Molecular Structure Kinase Organic Chemistry Amides digestive system diseases Enzyme assay 030104 developmental biology chemistry 030220 oncology & carcinogenesis biology.protein Molecular Medicine
Zdroj:	Bioorganicmedicinal chemistry letters. 26(11)
ISSN:	1464-3405
Popis:	The discovery and optimization of a series of indazole amide based extracellular signal-regulated kinase inhibitors via structure/knowledge based drug design and kinase screen is reported. The optimized compounds demonstrate potent inhibition of ERK1/2 enzyme activity, growth of BRAF mutant HT29 cells and ERK signaling in HT29 cells.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4aa295799cc80526d6e91f37cbea689d https://pubmed.ncbi.nlm.nih.gov/27106711 Zobrazit plný text záznamu Full Text from ScienceDirect