N-(3-(phenylcarbamoyl)arylpyrimidine)-5-carboxamides as potent and selective inhibitors of Lck: structure, synthesis and SAR

Autor:	Alan C. Cheng, Stephen Schneider, Joseph J. Nunes, Xiaotian Zhu, Paul Gallant, Erin F. DiMauro, Xin Huang, Vinod F. Patel, John Newcomb, Brian L. Hodous, Holly L. Deak, Christina Boucher, Susan M. Turci, Josie H. Lee, Linda F. Epstein
Rok vydání:	2007
Předmět:	Threonine medicine.drug_class Stereochemistry Clinical Biochemistry Molecular Conformation Pharmaceutical Science Carboxamide Crystallography X-Ray Biochemistry Chemical synthesis Structure-Activity Relationship Drug Discovery medicine Molecule Structure–activity relationship Transferase Combinatorial Chemistry Techniques Humans Molecular Biology chemistry.chemical_classification Molecular Structure Hydrogen bond Organic Chemistry Hydrogen Bonding Amides Enzyme Pyrimidines chemistry Lymphocyte Specific Protein Tyrosine Kinase p56(lck) Drug Design Molecular Medicine Selectivity
Zdroj:	Bioorganicmedicinal chemistry letters. 18(3)
ISSN:	1464-3405
Popis:	N-3-(Phenylcarbamoyl)arylpyrimidine-5-carboxamides are a novel class of selective Lck inhibitors. This series of compounds derives its selectivity from a hydrogen bond with the gatekeeper Thr316 of the enzyme. X-ray co-crystal structural data, structure-activity relationships, and the synthesis of these inhibitors are reported herein.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a79e72e4e6984650f09152ff1fcc2fe7 https://pubmed.ncbi.nlm.nih.gov/18083554 Zobrazit plný text záznamu Full Text from ScienceDirect