Literature DB >> 18426196

Discovery and optimization of triazolopyridazines as potent and selective inhibitors of the c-Met kinase.

Brian K Albrecht1, Jean-Christophe Harmange, David Bauer, Loren Berry, Christiane Bode, Alessandro A Boezio, April Chen, Deborah Choquette, Isabelle Dussault, Cary Fridrich, Satoko Hirai, Doug Hoffman, Jay F Larrow, Paula Kaplan-Lefko, Jasmine Lin, Julia Lohman, Alexander M Long, Jodi Moriguchi, Anne O'Connor, Michele H Potashman, Monica Reese, Karen Rex, Aaron Siegmund, Kavita Shah, Roman Shimanovich, Stephanie K Springer, Yohannes Teffera, Yajing Yang, Yihong Zhang, Steven F Bellon.   

Abstract

Tumorigenesis is a multistep process in which oncogenes play a key role in tumor formation, growth, and maintenance. MET was discovered as an oncogene that is activated by its ligand, hepatocyte growth factor. Deregulated signaling in the c-Met pathway has been observed in multiple tumor types. Herein we report the discovery of potent and selective triazolopyridazine small molecules that inhibit c-Met activity.

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Year:  2008        PMID: 18426196     DOI: 10.1021/jm800043g

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


  19 in total

1.  Energetic factors determining the binding of type I inhibitors to c-Met kinase: experimental studies and quantum mechanical calculations.

Authors:  Zhe Yu; Yu-chi Ma; Jing Ai; Dan-qi Chen; Dong-mei Zhao; Xin Wang; Yue-lei Chen; Mei-yu Geng; Bing Xiong; Mao-sheng Cheng; Jing-Kang Shen
Journal:  Acta Pharmacol Sin       Date:  2013-09-23       Impact factor: 6.150

2.  Pharmacophore modeling and virtual screening studies to identify new c-Met inhibitors.

Authors:  Wenting Tai; Tao Lu; Haoliang Yuan; Fengxiao Wang; Haichun Liu; Shuai Lu; Ying Leng; Weiwei Zhang; Yulei Jiang; Yadong Chen
Journal:  J Mol Model       Date:  2011-12-28       Impact factor: 1.810

3.  Structural basis for selective small molecule kinase inhibition of activated c-Met.

Authors:  Keith W Rickert; Sangita B Patel; Timothy J Allison; Noel J Byrne; Paul L Darke; Rachael E Ford; David J Guerin; Dawn L Hall; Maria Kornienko; Jun Lu; Sanjeev K Munshi; John C Reid; Jennifer M Shipman; Elizabeth F Stanton; Kevin J Wilson; Jonathon R Young; Stephen M Soisson; Kevin J Lumb
Journal:  J Biol Chem       Date:  2011-01-18       Impact factor: 5.157

Review 4.  Ten things you should know about protein kinases: IUPHAR Review 14.

Authors:  Doriano Fabbro; Sandra W Cowan-Jacob; Henrik Moebitz
Journal:  Br J Pharmacol       Date:  2015-03-24       Impact factor: 8.739

5.  Docking and quantitative structure-activity relationship studies for 3-fluoro-4-(pyrrolo[2,1-f][1,2,4]triazin-4-yloxy)aniline, 3-fluoro-4-(1H-pyrrolo[2,3-b]pyridin-4-yloxy)aniline, and 4-(4-amino-2-fluorophenoxy)-2-pyridinylamine derivatives as c-Met kinase inhibitors.

Authors:  Julio Caballero; Miguel Quiliano; Jans H Alzate-Morales; Mirko Zimic; Eric Deharo
Journal:  J Comput Aided Mol Des       Date:  2011-04-13       Impact factor: 3.686

6.  Imaging the Met Receptor Tyrosine Kinase (Met) and Assessing Tumor Responses to a Met Tyrosine Kinase Inhibitor in Human Xenograft Mouse Models with a [99mTc] (AH-113018) or Cy 5** (AH-112543) Labeled Peptide.

Authors:  Elaine M Jagoda; Sibaprasad Bhattacharyya; Joseph Kalen; Lisa Riffle; Avrum Leeder; Stephanie Histed; Mark Williams; Karen J Wong; Biying Xu; Lawrence P Szajek; Osama Elbuluk; Fabiola Cecchi; Kristen Raffensperger; Meghana Golla; Donald P Bottaro; Peter Choyke
Journal:  Mol Imaging       Date:  2015       Impact factor: 4.488

7.  Discovery of a novel mode of protein kinase inhibition characterized by the mechanism of inhibition of human mesenchymal-epithelial transition factor (c-Met) protein autophosphorylation by ARQ 197.

Authors:  Sudharshan Eathiraj; Rocio Palma; Erika Volckova; Marscha Hirschi; Dennis S France; Mark A Ashwell; Thomas C K Chan
Journal:  J Biol Chem       Date:  2011-03-24       Impact factor: 5.157

Review 8.  Tea catechins as inhibitors of receptor tyrosine kinases: mechanistic insights and human relevance.

Authors:  Christine A Larsen; Roderick H Dashwood; William H Bisson
Journal:  Pharmacol Res       Date:  2010-08-04       Impact factor: 7.658

9.  Tea catechins inhibit hepatocyte growth factor receptor (MET kinase) activity in human colon cancer cells: kinetic and molecular docking studies.

Authors:  Christine A Larsen; William H Bisson; Roderick H Dashwood
Journal:  J Med Chem       Date:  2009-11-12       Impact factor: 7.446

Review 10.  Cancer driver mutations in protein kinase genes.

Authors:  Ali Torkamani; Gennady Verkhivker; Nicholas J Schork
Journal:  Cancer Lett       Date:  2008-12-10       Impact factor: 8.679

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