Literature DB >> 21733693

Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup.

John C Stellwagen1, George M Adjabeng, Marc R Arnone, Scott H Dickerson, Chao Han, Keith R Hornberger, Alastair J King, Robert A Mook, Kimberly G Petrov, Tara R Rheault, Cynthia M Rominger, Olivia W Rossanese, Kimberly N Smitheman, Alex G Waterson, David E Uehling.   

Abstract

A potent series of inhibitors against the B-Raf(V600E) kinase have been developed that show excellent activity in cellular assays and good oral bioavailability in rats. The key structural features of the series are an arylsulfonamide headgroup, a thiazole core, and a fluorine ortho to the sulfonamide nitrogen. Crown
Copyright © 2011. Published by Elsevier Ltd. All rights reserved.

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Year:  2011        PMID： 21733693     DOI： 10.1016/j.bmcl.2011.06.021

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


  6 in total

1.  Analysis of B-Raf[Formula: see text] inhibitors using 2D and 3D-QSAR, molecular docking and pharmacophore studies.

Authors:  Reza Aalizadeh; Eslam Pourbasheer; Mohammad Reza Ganjali
Journal:  Mol Divers       Date:  2015-08-15       Impact factor: 2.943

2.  EGFR inhibitors identified as a potential treatment for chordoma in a focused compound screen.

Authors:  Susanne Scheipl; Michelle Barnard; Lucia Cottone; Mette Jorgensen; David H Drewry; William J Zuercher; Fabrice Turlais; Hongtao Ye; Ana P Leite; James A Smith; Andreas Leithner; Peter Möller; Silke Brüderlein; Naomi Guppy; Fernanda Amary; Roberto Tirabosco; Sandra J Strauss; Nischalan Pillay; Adrienne M Flanagan
Journal:  J Pathol       Date:  2016-05-31       Impact factor: 7.996

3.  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

4.  Trisubstituted thiazoles as potent and selective inhibitors of Plasmodium falciparum protein kinase G (PfPKG).

Authors:  Denise J Tsagris; Kristian Birchall; Nathalie Bouloc; Jonathan M Large; Andy Merritt; Ela Smiljanic-Hurley; Mary Wheldon; Keith H Ansell; Catherine Kettleborough; David Whalley; Lindsay B Stewart; Paul W Bowyer; David A Baker; Simon A Osborne
Journal:  Bioorg Med Chem Lett       Date:  2018-08-27       Impact factor: 2.823

5.  Discovery of Dabrafenib: A Selective Inhibitor of Raf Kinases with Antitumor Activity against B-Raf-Driven Tumors.

Authors:  Tara R Rheault; John C Stellwagen; George M Adjabeng; Keith R Hornberger; Kimberly G Petrov; Alex G Waterson; Scott H Dickerson; Robert A Mook; Sylvie G Laquerre; Alastair J King; Olivia W Rossanese; Marc R Arnone; Kimberly N Smitheman; Laurie S Kane-Carson; Chao Han; Ganesh S Moorthy; Katherine G Moss; David E Uehling
Journal:  ACS Med Chem Lett       Date:  2013-02-07       Impact factor: 4.345

Review 6.  Structural simplification: an efficient strategy in lead optimization.

Authors:  Shengzheng Wang; Guoqiang Dong; Chunquan Sheng
Journal:  Acta Pharm Sin B       Date:  2019-06-06       Impact factor: 11.413
  6 in total

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