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.

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22024030 [ View in PubMed

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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

Drug	Target	Property	Measurement	pH	Temperature (°C)
Sorafenib	Serine/threonine-protein kinase B-raf	IC 50 (nM)	22	N/A	N/A	Details