Novel thienopyrimidine and thiazolopyrimidine kinase inhibitors with activity against Tie-2 in vitro and in vivo

The SAR and improvement in potency against Tie-2 of novel thienopyrimidine and thiazolopyrimidine kinase inhibitors are reported. These compounds have moderate potency in cellular assays of Tie-2 inhibition, good physical properties, DMPK, and show evidence of in vivo inhibition of Tie-2. The SAR an...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2009-12, Vol.19 (23), p.6670-6674
Hauptverfasser:	Luke, Richard W.A., Ballard, Peter, Buttar, David, Campbell, Leonie, Curwen, Jon, Emery, Steve C., Griffen, Alison M., Hassall, Lorraine, Hayter, Barry R., Jones, Cliff D., McCoull, William, Mellor, Martine, Swain, Mike L., Tucker, Julie A.
Format:	Artikel
Sprache:	eng
Schlagworte:	Angiogenesis Antineoplastic agents Biological and medical sciences Crystallography, X-Ray Drug Design General aspects Humans Inhibition Kinase Medical sciences Models, Molecular Molecular Structure Pharmacology. Drug treatments Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Pyrimidines - chemical synthesis Pyrimidines - chemistry Pyrimidines - pharmacology Receptor, TIE-2 - antagonists & inhibitors Small molecule Stereoisomerism Structure-Activity Relationship TEK Thiazoles - chemical synthesis Thiazoles - chemistry Thiazoles - pharmacology Tie-2
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