Discovery of novel imidazo[1,2-a]pyrazin-8-amines as Brk/PTK6 inhibitors

Autor:	Yan Wang, Patrick J. Curran, Jack B. Bracken, Gerald W. Shipps, M. Arshad Siddiqui, Hua Miao, David B. Belanger, Hongbo Zeng, Michael Malkowski
Rok vydání:	2011
Předmět:	Clinical Biochemistry High selectivity Dasatinib Pharmaceutical Science Breast Neoplasms Protein Serine-Threonine Kinases Biochemistry Inhibitory Concentration 50 Mice Structure-Activity Relationship Aurora Kinases Proto-Oncogenes Drug Discovery medicine Animals Humans Structure–activity relationship Computer Simulation Molecular Targeted Therapy Protein Kinase Inhibitors Molecular Biology Adaptor Proteins Signal Transducing Dose-Response Relationship Drug Chemistry Kinase Drug discovery Organic Chemistry Imidazoles RNA-Binding Proteins Signal transducing adaptor protein Oncogenes Protein-Tyrosine Kinases Neoplasm Proteins DNA-Binding Proteins Thiazoles Phenotype Pyrimidines Drug Design Pyrazines Melanocytes Molecular Medicine Female PTK6 Drug Screening Assays Antitumor Tyrosine kinase medicine.drug
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 21:5870-5875
ISSN:	0960-894X
Popis:	A series of substituted imidazo[1,2-a]pyrazin-8-amines were discovered as novel breast tumor kinase (Brk)/protein tyrosine kinase 6 (PTK6) inhibitors. Tool compounds with low-nanomolar Brk inhibition activity, high selectivity towards other kinases and desirable DMPK properties were achieved to enable the exploration of Brk as an oncology target.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c602c45bbeb7b8ec30580b6a5d7bc119 https://doi.org/10.1016/j.bmcl.2011.07.101 Zobrazit plný text záznamu Full Text from ScienceDirect