Literature DB >> 16420026

Potent and selective mitogen-activated protein kinase kinase (MEK) 1,2 inhibitors. 1. 4-(4-bromo-2-fluorophenylamino)-1- methylpyridin-2(1H)-ones.

Eli M Wallace1, Joseph Lyssikatos, James F Blake, Jeongbeob Seo, Hong Woon Yang, Tammie C Yeh, Michele Perrier, Heidi Jarski, Vivienne Marsh, Gregory Poch, Michelle Goyette Livingston, Jennifer Otten, Gary Hingorani, Rich Woessner, Patrice Lee, James Winkler, Kevin Koch.   

Abstract

The role of MEK 1,2 in cancer tumorgenesis has been clearly demonstrated preclinically, and two selective inhibitors are currently undergoing clinical evaluation to determine their role in the human disease. We have discovered 4-(4-bromo-2-fluorophenylamino)-1-methylpyridin-2(1H)-ones as a new class of ATP noncompetitive MEK inhibitors. These inhibitors exhibit excellent cellular potency and good pharmacokinetic properties and have demonstrated the ability to inhibit ERK phosphorylation in HT-29 tumors from mouse xenograft studies.

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Year:  2006        PMID： 16420026     DOI： 10.1021/jm050834y

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  8 in total

1.  Novel Nitric Oxide Donors of Phenylsulfonylfuroxan and 3-Benzyl Coumarin Derivatives as Potent Antitumor Agents.

Authors:  Yalan Guo; Yujie Wang; Haihong Li; Ke Wang; Qi Wan; Jia Li; Yubo Zhou; Ying Chen
Journal:  ACS Med Chem Lett       Date:  2018-04-20       Impact factor: 4.345

2.  Pyrazolopyridine Inhibitors of B-Raf(V600E). Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors.

Authors:  Steve Wenglowsky; Li Ren; Kateri A Ahrendt; Ellen R Laird; Ignacio Aliagas; Bruno Alicke; Alex J Buckmelter; Edna F Choo; Victoria Dinkel; Bainian Feng; Susan L Gloor; Stephen E Gould; Stefan Gross; Janet Gunzner-Toste; Joshua D Hansen; Georgia Hatzivassiliou; Bonnie Liu; Kim Malesky; Simon Mathieu; Brad Newhouse; Nicholas J Raddatz; Yingqing Ran; Sumeet Rana; Nikole Randolph; Tyler Risom; Joachim Rudolph; Scott Savage; LeAnn T Selby; Michael Shrag; Kyung Song; Hillary L Sturgis; Walter C Voegtli; Zhaoyang Wen; Brandon S Willis; Richard D Woessner; Wen-I Wu; Wendy B Young; Jonas Grina
Journal:  ACS Med Chem Lett       Date:  2011-03-08       Impact factor: 4.345

3.  Discovery of a Highly Potent and Selective MEK Inhibitor: GSK1120212 (JTP-74057 DMSO Solvate).

Authors:  Hiroyuki Abe; Shinichi Kikuchi; Kazuhide Hayakawa; Tetsuya Iida; Noboru Nagahashi; Katsuya Maeda; Johei Sakamoto; Noriaki Matsumoto; Tomoya Miura; Koji Matsumura; Noriyoshi Seki; Takashi Inaba; Hisashi Kawasaki; Takayuki Yamaguchi; Reina Kakefuda; Toyomichi Nanayama; Hironori Kurachi; Yoshikazu Hori; Takayuki Yoshida; Junya Kakegawa; Yoshihiro Watanabe; Aidan G Gilmartin; Mark C Richter; Katherine G Moss; Sylvie G Laquerre
Journal:  ACS Med Chem Lett       Date:  2011-02-28       Impact factor: 4.345

4.  RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth.

Authors:  Georgia Hatzivassiliou; Kyung Song; Ivana Yen; Barbara J Brandhuber; Daniel J Anderson; Ryan Alvarado; Mary J C Ludlam; David Stokoe; Susan L Gloor; Guy Vigers; Tony Morales; Ignacio Aliagas; Bonnie Liu; Steve Sideris; Klaus P Hoeflich; Bijay S Jaiswal; Somasekar Seshagiri; Hartmut Koeppen; Marcia Belvin; Lori S Friedman; Shiva Malek
Journal:  Nature       Date:  2010-02-03       Impact factor: 49.962

5.  Efficient and divergent synthesis of polyfunctionalized 2-pyridones from β-keto amides.

Authors:  Baochang Gao; Yufeng Sun; Jun Wang; Zhigang Yuan; Liwu Zu; Xu Zhang; Wenbin Liu
Journal:  RSC Adv       Date:  2018-10-01       Impact factor: 4.036

6.  LAT1 activity of carboxylic acid bioisosteres: Evaluation of hydroxamic acids as substrates.

Authors:  Arik A Zur; Huan-Chieh Chien; Evan Augustyn; Andrew Flint; Nathan Heeren; Karissa Finke; Christopher Hernandez; Logan Hansen; Sydney Miller; Lawrence Lin; Kathleen M Giacomini; Claire Colas; Avner Schlessinger; Allen A Thomas
Journal:  Bioorg Med Chem Lett       Date:  2016-09-03       Impact factor: 2.823

7.  Colorectal cancer cells with the BRAF(V600E) mutation are addicted to the ERK1/2 pathway for growth factor-independent survival and repression of BIM.

Authors:  J A Wickenden; H Jin; M Johnson; A S Gillings; C Newson; M Austin; S D Chell; K Balmanno; C A Pritchard; S J Cook
Journal:  Oncogene       Date:  2008-09-22       Impact factor: 9.867

8.  Binding modes of three inhibitors 8CA, F8A and I4A to A-FABP studied based on molecular dynamics simulation.

Authors:  Jianzhong Chen; Jinan Wang; Weiliang Zhu
Journal:  PLoS One       Date:  2014-06-11       Impact factor: 3.240
  8 in total

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