Structure–activity relationship studies of imidazo[1,2- c]pyrimidine derivatives as potent and orally effective Syk family kinases inhibitors

The conversion of 1,2,4-triazolo[4,3- c]pyrimidine to a imidazo[1,2- c]pyrimidine derivative improves in vivo efficacy of suppression of both passive cutaneous anaphylaxis (PCA) reaction and ConA-induced IL-2 production. Additionally, the inhibitory effects of the derivatives on Syk family kinase ac...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2008-10, Vol.16 (20), p.9247-9260
Hauptverfasser:	Hirabayashi, Akihito, Mukaiyama, Harunobu, Kobayashi, Hiroaki, Shiohara, Hiroaki, Nakayama, Satoko, Ozawa, Motoyasu, Tsuji, Eiichi, Miyazawa, Keiji, Misawa, Keiko, Ohnota, Hideki, Isaji, Masayuki
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Animals Autoimmune diseases Biological and medical sciences Crystallography, X-Ray Enzyme Activation - drug effects Humans Imidazoles - chemistry Immunomodulators Inhibitory Concentration 50 Intracellular Signaling Peptides and Proteins - antagonists & inhibitors Intracellular Signaling Peptides and Proteins - classification Intracellular Signaling Peptides and Proteins - metabolism Medical sciences Mice Mice, Inbred ICR Models, Molecular Molecular Structure Pharmacology. Drug treatments Protein Kinase Inhibitors - administration & dosage Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - chemistry Protein tyrosine kinases (PTKs) Protein-Tyrosine Kinases - antagonists & inhibitors Protein-Tyrosine Kinases - classification Protein-Tyrosine Kinases - metabolism Pyrimidines - administration & dosage Pyrimidines - chemical synthesis Pyrimidines - chemistry Structure-Activity Relationship Syk Syk and/or ZAP-70 kinase inhibitor Syk family kinases Syk Kinase ZAP-70 ZAP-70 Protein-Tyrosine Kinase - antagonists & inhibitors ZAP-70 Protein-Tyrosine Kinase - metabolism
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