Structure-based design of isoindoline-1,3-diones and 2,3-dihydrophthalazine-1,4-diones as novel B-Raf inhibitors.
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Wang X, Salaski EJ, Berger DM, Powell D, Hu Y, Wojciechowicz D, Collins K, Frommer E
Structure-based design of isoindoline-1,3-diones and 2,3-dihydrophthalazine-1,4-diones as novel B-Raf inhibitors.
Bioorg Med Chem Lett. 2011 Dec 1;21(23):6941-4. doi: 10.1016/j.bmcl.2011.10.012. Epub 2011 Oct 12.
- PubMed ID
- 22024030 [ View in PubMed]
- Abstract
Structure-guided design led to the discovery of novel chemical scaffolds for B-Raf inhibitors. Both type I and type II kinase inhibitors have been explored and lead compounds with good potency and excellent selectivity have been identified.
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- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Sorafenib Serine/threonine-protein kinase B-raf IC 50 (nM) 22 N/A N/A Details