Synthesis of an aryloxy oxo pyrimidinone library that displays ALK-selective inhibition.
Article Details
- CitationCopy to clipboard
Slavish PJ, Price JE, Jiang Q, Cui X, Morris SW, Webb TR
Synthesis of an aryloxy oxo pyrimidinone library that displays ALK-selective inhibition.
Bioorg Med Chem Lett. 2011 Aug 1;21(15):4592-6. doi: 10.1016/j.bmcl.2011.05.103. Epub 2011 Jun 12.
- PubMed ID
- 21708465 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Crizotinib Hepatocyte growth factor receptor IC 50 (nM) 0.78 N/A N/A Details