Structure-activity relationships of a novel class of Src SH2 inhibitors

Autor:	Kara A. Loiacono, Ian A. MacNeil, Berkley A. Lynch, Taylor Merry, Chi B. Vu, Ukti Mani, Vaibhav Varkhedkar, John L. Buchanan, Dennis A. Holt, Selvaluxmi G. Pradeepan, Hilary R. Plake, Michael Yang, Evelyn G. Corpuz, Choi Lai Tiong
Rok vydání:	1999
Předmět:	chemistry.chemical_classification Tetrapeptide Chemistry Stereochemistry Organic Chemistry Clinical Biochemistry Pharmaceutical Science SH2 domain Biochemistry Chemical synthesis In vitro src Homology Domains Structure-Activity Relationship Thiazoles Enzyme Drug Discovery Side chain Molecular Medicine Structure–activity relationship Molecular Biology Proto-oncogene tyrosine-protein kinase Src
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 9:2359-2364
ISSN:	0960-894X
DOI:	10.1016/s0960-894x(99)00389-3
Popis:	The structure-activity relationships (SAR) of a novel class of Src SH2 inhibitors are described. Variation at the pY+1 and pY+3 side chain positions using 2,4- and 2,5-substituted thiazoles and 1,2,4-oxadiazoles as scaffolds resulted in inhibitors that bound as well as the standard tetrapeptide Ac-pYEEI-NH2.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3e24c3271625ce90015f47df8c67738d https://doi.org/10.1016/s0960-894x(99)00389-3 Zobrazit plný text záznamu Full Text from ScienceDirect