Literature DB >> 23489628

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

Yunfeng Xie1, Xianjie Chen, Jie Qin, Xiangqian Kong, Fei Ye, Yuren Jiang, Hong Liu, Hualiang Jiang, Ronen Marmorstein, Cheng Luo.   

Abstract

The V600E BRAF kinase mutation, which activates the downstream MAPK signaling pathway, commonly occurs in about 8% of all human malignancies and about 50% of all melanomas. In this study, we employed virtual screening and chemical synthesis to identify a series of N-(thiophen-2-yl) benzamide derivatives as potent BRAF(V600E) inhibitors. Structure-activity relationship studies of these derivatives revealed that compounds b40 and b47 are the two most potent BRAF(V600E) inhibitors in this series.
Copyright © 2013 Elsevier Ltd. All rights reserved.

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Year:  2013        PMID： 23489628      PMCID： PMC4026330          DOI： 10.1016/j.bmcl.2013.02.072

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


  28 in total

Review 1.  Mitogen-activated protein kinase pathways.

Authors:  M J Robinson; M H Cobb
Journal:  Curr Opin Cell Biol       Date:  1997-04       Impact factor: 8.382

2.  Development of a novel class of B-Raf(V600E)-selective inhibitors through virtual screening and hierarchical hit optimization.

Authors:  Xiangqian Kong; Jie Qin; Zeng Li; Adina Vultur; Linjiang Tong; Enguang Feng; Geena Rajan; Shien Liu; Junyan Lu; Zhongjie Liang; Mingyue Zheng; Weiliang Zhu; Hualiang Jiang; Meenhard Herlyn; Hong Liu; Ronen Marmorstein; Cheng Luo
Journal:  Org Biomol Chem       Date:  2012-09-28       Impact factor: 3.876

3.  Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors. 1. Exploration of [5,6]-fused bicyclic scaffolds.

Authors:  Masanori Okaniwa; Masaaki Hirose; Takashi Imada; Tomohiro Ohashi; Youko Hayashi; Tohru Miyazaki; Takeo Arita; Masato Yabuki; Kazuyo Kakoi; Juran Kato; Terufumi Takagi; Tomohiro Kawamoto; Shuhei Yao; Akihiko Sumita; Shunichirou Tsutsumi; Tsuneaki Tottori; Hideyuki Oki; Bi-Ching Sang; Jason Yano; Kathleen Aertgeerts; Sei Yoshida; Tomoyasu Ishikawa
Journal:  J Med Chem       Date:  2012-03-14       Impact factor: 7.446

4.  Lead- and drug-like compounds: the rule-of-five revolution.

Authors:  Christopher A Lipinski
Journal:  Drug Discov Today Technol       Date:  2004-12

5.  4-Quinazolinyloxy-diaryl ureas as novel BRAFV600E inhibitors.

Authors:  Mark W Holladay; 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
Journal:  Bioorg Med Chem Lett       Date:  2011-07-14       Impact factor: 2.823

6.  Selective BRAFV600E inhibition enhances T-cell recognition of melanoma without affecting lymphocyte function.

Authors:  Andrea Boni; Alexandria P Cogdill; Ping Dang; Durga Udayakumar; Ching-Ni Jenny Njauw; Callum M Sloss; Cristina R Ferrone; Keith T Flaherty; Donald P Lawrence; David E Fisher; Hensin Tsao; Jennifer A Wargo
Journal:  Cancer Res       Date:  2010-06-15       Impact factor: 12.701

7.  Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity.

Authors:  James Tsai; John T Lee; Weiru Wang; Jiazhong Zhang; Hanna Cho; Shumeye Mamo; Ryan Bremer; Sam Gillette; Jun Kong; Nikolas K Haass; Katrin Sproesser; Ling Li; Keiran S M Smalley; Daniel Fong; Yong-Liang Zhu; Adhirai Marimuthu; Hoa Nguyen; Billy Lam; Jennifer Liu; Ivana Cheung; Julie Rice; Yoshihisa Suzuki; Catherine Luu; Calvin Settachatgul; Rafe Shellooe; John Cantwell; Sung-Hou Kim; Joseph Schlessinger; Kam Y J Zhang; Brian L West; Ben Powell; Gaston Habets; Chao Zhang; Prabha N Ibrahim; Peter Hirth; Dean R Artis; Meenhard Herlyn; Gideon Bollag
Journal:  Proc Natl Acad Sci U S A       Date:  2008-02-19       Impact factor: 11.205

8.  Molecular shape and medicinal chemistry: a perspective.

Authors:  Anthony Nicholls; Georgia B McGaughey; Robert P Sheridan; Andrew C Good; Gregory Warren; Magali Mathieu; Steven W Muchmore; Scott P Brown; J Andrew Grant; James A Haigh; Neysa Nevins; Ajay N Jain; Brian Kelley
Journal:  J Med Chem       Date:  2010-05-27       Impact factor: 7.446

9.  Identification of BRAF inhibitors through in silico screening.

Authors:  Cheng Luo; Peng Xie; Ronen Marmorstein
Journal:  J Med Chem       Date:  2008-09-11       Impact factor: 7.446

10.  Making sense of MEK1 mutations in intrinsic and acquired BRAF inhibitor resistance.

Authors:  Kim H T Paraiso; Keiran S M Smalley
Journal:  Cancer Discov       Date:  2012-05       Impact factor: 39.397
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