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Structure-based discovery of C-2 substituted imidazo-pyrrolopyridine JAK1 inhibitors with improved selectivity over JAK2
Bioorganic & medicinal chemistry letters, 2012-12, Vol.22 (24), p.7627-7633
2012

Details

Autor(en) / Beteiligte
Titel
Structure-based discovery of C-2 substituted imidazo-pyrrolopyridine JAK1 inhibitors with improved selectivity over JAK2
Ist Teil von
  • Bioorganic & medicinal chemistry letters, 2012-12, Vol.22 (24), p.7627-7633
Ort / Verlag
Amsterdam: Elsevier Ltd
Erscheinungsjahr
2012
Link zum Volltext
Quelle
MEDLINE
Beschreibungen/Notizen
  • Herein we describe our successful efforts in obtaining C-2 substituted imidazo-pyrrolopyridines with improved JAK1 selectivity relative to JAK2 by targeting an amino acid residue that differs between the two isoforms (JAK1: E966; JAK2: D939). Efforts to improve cellular potency by reducing the polarity of the inhibitors are also detailed. The X-ray crystal structure of a representative inhibitor in complex with the JAK1 enzyme is also disclosed.
Sprache
Englisch
Identifikatoren
ISSN: 0960-894X
eISSN: 1464-3405
DOI: 10.1016/j.bmcl.2012.10.008
Titel-ID: cdi_proquest_miscellaneous_1272726307
Format
–
Schlagworte
Amino acids, Animals, Biological and medical sciences, Bones, joints and connective tissue. Antiinflammatory agents, chemistry, Crystal structure, Crystallography, X-Ray, Dose-Response Relationship, Drug, Drug Discovery, Enzymes, Humans, Imidazo-pyrrolopyridines, Imidazoles - chemistry, Ionizing radiation, JAK1 selective inhibitors, Janus kinase, Janus Kinase 1 - antagonists & inhibitors, Janus Kinase 1 - metabolism, Janus kinase 2, Janus Kinase 2 - antagonists & inhibitors, Janus Kinase 2 - metabolism, Male, Medical sciences, Models, Molecular, Molecular Structure, Pharmacology. Drug treatments, Polarity, Protein Kinase Inhibitors - administration & dosage, Protein Kinase Inhibitors - chemistry, Protein Kinase Inhibitors - pharmacology, Pyridines - administration & dosage, Pyridines - chemistry, Pyridines - pharmacology, Pyrroles - administration & dosage, Pyrroles - chemistry, Pyrroles - pharmacology, Rats, Rats, Sprague-Dawley, Rheumatoid arthritis, Structure-Activity Relationship, Structure-based design, X-ray diffraction

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