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Synthesis of an aryloxy oxo pyrimidinone library that displays ALK-selective inhibition.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2011 Aug 01; Vol. 21 (15), pp. 4592-6. Date of Electronic Publication: 2011 Jun 12. - Publication Year :
- 2011
-
Abstract
- We report the synthesis of a pyrimidinone library that targets anaplastic lymphoma kinase (ALK), an oncogenic receptor tyrosine kinase. This library was generated in three steps from a versatile commercially available starting material. Some compounds within this library showed single digit micromolar inhibition of ALK in vitro, while showing minimal inhibition of other homologous insulin receptor family kinases including the human insulin receptor kinase (IRK), at the highest concentrations investigated. We also present initial ALK structure-activity relationships for this library.<br /> (Copyright © 2011 Elsevier Ltd. All rights reserved.)
- Subjects :
- Anaplastic Lymphoma Kinase
Antigens, CD metabolism
Humans
Protein Kinase Inhibitors chemistry
Protein Kinase Inhibitors pharmacology
Pyrimidinones chemical synthesis
Pyrimidinones pharmacology
Receptor Protein-Tyrosine Kinases metabolism
Receptor, Insulin antagonists & inhibitors
Receptor, Insulin metabolism
Structure-Activity Relationship
Protein Kinase Inhibitors chemical synthesis
Pyrimidinones chemistry
Receptor Protein-Tyrosine Kinases antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 21
- Issue :
- 15
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 21708465
- Full Text :
- https://doi.org/10.1016/j.bmcl.2011.05.103