3-Amino-pyrazolo[3,4-d]pyrimidines as p38α kinase inhibitors: Design and development to a highly selective lead

Learnings from previous Roche p38-selective inhibitors were applied to a new fragment hit, which was optimized to a potent, exquisitely selective preclinical lead with a good pharmacokinetic profile.

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2011-06, Vol.21 (11), p.3452-3456
Hauptverfasser:	Soth, Michael, Abbot, Sarah, Abubakari, Allassan, Arora, Nidhi, Arzeno, Humberto, Billedeau, Roland, Dewdney, Nolan, Durkin, Kieran, Frauchiger, Sandra, Ghate, Manjiri, Goldstein, David M., Hill, Ronald J., Kuglstatter, Andreas, Li, Fujun, Loe, Brad, McCaleb, Kristen, McIntosh, Joel, Papp, Eva, Park, Jaehyeon, Stahl, Martin, Sung, Man-Ling, Suttman, Rebecca, Swinney, David C., Weller, Paul, Wong, Brian, Zecic, Hasim, Gabriel, Tobias
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Crystallography, X-Ray Drug Design Enzyme Activation - drug effects Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Inhibitory Concentration 50 Kinase Kinase inhibitor Medical sciences Mitogen-Activated Protein Kinase 14 - antagonists & inhibitors Models, Molecular Molecular Structure p38 Pharmacology. Drug treatments Pyrazoles - chemical synthesis Pyrazoles - chemistry Pyrazoles - pharmacology Pyrimidines - chemical synthesis Pyrimidines - chemistry Pyrimidines - pharmacology Rats
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Beschreibung
Zusammenfassung:	Learnings from previous Roche p38-selective inhibitors were applied to a new fragment hit, which was optimized to a potent, exquisitely selective preclinical lead with a good pharmacokinetic profile.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2011.03.098