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Bioorg Med Chem Lett. 2011 Sep 15;21(18):5342-6. doi: 10.1016/j.bmcl.2011.07.019. Epub 2011 Jul 14.

4-Quinazolinyloxy-diaryl ureas as novel BRAFV600E inhibitors.

Author information

1
Ambit Biosciences Corporation, 4215 Sorrento Valley Boulevard, San Diego, CA 92121, USA. mholladay@ambitbio.com

Abstract

Aryl phenyl ureas with a 4-quinazolinoxy substituent at the meta-position of the phenyl ring are potent inhibitors of mutant and wild type BRAF kinase. Compound 7 (1-(5-tert-butylisoxazol-3-yl)-3-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)urea hydrochloride) exhibits good pharmacokinetic properties in rat and mouse and is efficacious in a mouse tumor xenograft model following oral dosing.

PMID:
21807507
DOI:
10.1016/j.bmcl.2011.07.019
[Indexed for MEDLINE]

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