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Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs).
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2009 Oct 15; Vol. 19 (20), pp. 5887-92. Date of Electronic Publication: 2009 Aug 23. - Publication Year :
- 2009
-
Abstract
- A series of phenylaminopyrimidines has been identified as inhibitors of Janus kinases (JAKs). Development of this initial series led to the potent JAK2/JAK1 inhibitor CYT387 (N-(cyanomethyl)-4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]-benzamide). Details of synthesis and SAR studies of these compounds are reported.
- Subjects :
- Animals
Benzamides chemical synthesis
Benzamides pharmacology
Binding Sites
Caco-2 Cells
Cell Line, Tumor
Computer Simulation
Humans
Janus Kinase 2 metabolism
Male
Protein Isoforms antagonists & inhibitors
Protein Isoforms metabolism
Protein Kinase Inhibitors chemical synthesis
Protein Kinase Inhibitors pharmacokinetics
Pyrimidines chemical synthesis
Pyrimidines pharmacokinetics
Pyrimidines pharmacology
Rats
Rats, Sprague-Dawley
Structure-Activity Relationship
Benzamides chemistry
Janus Kinase 2 antagonists & inhibitors
Protein Kinase Inhibitors chemistry
Pyrimidines chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 19
- Issue :
- 20
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 19762238
- Full Text :
- https://doi.org/10.1016/j.bmcl.2009.08.071