Literature DB >> 21807507

4-Quinazolinyloxy-diaryl ureas as novel BRAFV600E inhibitors.

Mark W Holladay1, Brian T Campbell, Martin W Rowbottom, Qi Chao, Kelly G Sprankle, Andiliy G Lai, Sunny Abraham, Eduardo Setti, Raffaella Faraoni, Lan Tran, Robert C Armstrong, Ruwanthi N Gunawardane, Michael F Gardner, Merryl D Cramer, Dana Gitnick, Mark A Ator, Bruce D Dorsey, Bruce R Ruggeri, Michael Williams, Shripad S Bhagwat, Joyce James.   

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.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID: 21807507     DOI: 10.1016/j.bmcl.2011.07.019

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

1.  Antitumor Activity of RXDX-105 in Multiple Cancer Types with RET Rearrangements or Mutations.

Authors:  Gang G Li; Romel Somwar; James Joseph; Roger S Smith; Takuo Hayashi; Leenus Martin; Aleksandra Franovic; Anni Schairer; Eric Martin; Gregory J Riely; Jason Harris; Shunqi Yan; Ge Wei; Jennifer W Oliver; Rupal Patel; Pratik Multani; Marc Ladanyi; Alexander Drilon
Journal:  Clin Cancer Res       Date:  2016-12-23       Impact factor: 12.531

2.  Identification and synthesis of N-(thiophen-2-yl) benzamide derivatives as BRAF(V600E) inhibitors.

Authors:  Yunfeng Xie; Xianjie Chen; Jie Qin; Xiangqian Kong; Fei Ye; Yuren Jiang; Hong Liu; Hualiang Jiang; Ronen Marmorstein; Cheng Luo
Journal:  Bioorg Med Chem Lett       Date:  2013-02-26       Impact factor: 2.823

3.  Hexachlorocyclotriphosphazene (HCCP)-mediated direct formation of thioethers and ethers from quinazolin-4(3H)-ones.

Authors:  Baoxiang Hu; Xiaochu Zhang; Lili Sheng; Ming Guo; Zhenlu Shen; Xinquan Hu; Nan Sun; Weimin Mo
Journal:  Molecules       Date:  2013-05-15       Impact factor: 4.411

  3 in total

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