Structure-based design of isoindoline-1,3-diones and 2,3-dihydrophthalazine-1,4-diones as novel B-Raf inhibitors.

Article Details

Citation

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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
SorafenibSerine/threonine-protein kinase B-rafIC 50 (nM)22N/AN/ADetails