Bioorganic & medicinal chemistry letters, 2010-08, Vol.20 (16), p.4885-4891
2010
Volltextzugriff (PDF)
Details
- Autor(en) / Beteiligte
- Titel
- Enhanced selectivity profile of pyrazole-urea based DFG-out p38alpha inhibitors
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2010-08, Vol.20 (16), p.4885-4891
- Ort / Verlag
- England
- Erscheinungsjahr
- 2010
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- By targeting an extended region of the conventional 'DFG-out' pocket of p38alpha, while minimizing interactions with the specificity pocket and eliminating interactions with the adenine binding site, we are able to design and synthesize a number of pyrazole-urea based DFG-out p38alpha inhibitors with good potencies, and excellent selectivity.
- Sprache
- Englisch
- Identifikatoren
- eISSN: 1464-3405DOI: 10.1016/j.bmcl.2010.06.073Titel-ID: cdi_proquest_miscellaneous_749024175
- Format
- –
- Schlagworte
- Adenine - metabolism, Amino Acid Motifs, Amino Acid Sequence, Binding Sites, Humans, Microsomes - metabolism, Mitogen-Activated Protein Kinase 14 - antagonists & inhibitors, Mitogen-Activated Protein Kinase 14 - metabolism, Phenylurea Compounds - chemical synthesis, Phenylurea Compounds - chemistry, Phenylurea Compounds - pharmacology, Protein Kinase Inhibitors - chemistry, Protein Kinase Inhibitors - pharmacology, Pyrazoles - chemical synthesis, Pyrazoles - chemistry, Pyrazoles - pharmacology, Structure-Activity Relationship