Discovery of indazoles as inhibitors of Tpl2 kinase

Autor:	Yike Ni, Derek C. Cole, Rajiah Aldrin Denny, Julie Liu, David R. Anderson, Timothy Chamberlain, Yonghan Hu, Lih-Ling Lin, Manus Ipek, J. Perry Hall, Suvit Thaisrivongs, Michael Luong, Xiaolun Wang, Jean-Baptiste Telliez, Ariamala Gopalsamy
Rok vydání:	2011
Předmět:	MAPK/ERK pathway Models Molecular Indazoles Stereochemistry Clinical Biochemistry Pharmaceutical Science Biochemistry Monocytes chemistry.chemical_compound Structure-Activity Relationship Proto-Oncogene Proteins Drug Discovery Potency Humans Enzyme Inhibitors Molecular Biology Indazole Dose-Response Relationship Drug Molecular Structure Chemistry Kinase Organic Chemistry Stereoisomerism MAP Kinase Kinase Kinases Molecular Medicine
Zdroj:	Bioorganicmedicinal chemistry letters. 21(16)
ISSN:	1464-3405
Popis:	Synthesis, modeling and structure–activity relationship of indazoles as inhibitors of Tpl2 kinase are described. From a high throughput screening effort, we identified an indazole hit compound 5 that has a single digit micromolar Tpl2 activity. Through SAR modifications at the C3 and C5 positions of the indazole, we discovered compound 31 with good potency in LANCE assay and cell-based p -Erk assay.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a8d2b86d142711063633b691cd00acc5 https://pubmed.ncbi.nlm.nih.gov/21742493 Zobrazit plný text záznamu Full Text from ScienceDirect