Literature DB >> 26812066

Discovery of (R)-6-(1-(8-Fluoro-6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one (AMG 337), a Potent and Selective Inhibitor of MET with High Unbound Target Coverage and Robust In Vivo Antitumor Activity.

Alessandro A Boezio1, Katrina W Copeland1, Karen Rex2, Brian K Albrecht1, David Bauer1, Steven F Bellon1, Christiane Boezio1, Martin A Broome2, Deborah Choquette1, Angela Coxon2, Isabelle Dussault2, Satoko Hirai1, Richard Lewis1, Min-Hwa Jasmine Lin1, Julia Lohman1, Jingzhou Liu1, Emily A Peterson1, Michele Potashman1, Roman Shimanovich1, Yohannes Teffera1, Douglas A Whittington1, Karina R Vaida1, Jean-Christophe Harmange1.   

Abstract

Deregulation of the receptor tyrosine kinase mesenchymal epithelial transition factor (MET) has been implicated in several human cancers and is an attractive target for small molecule drug discovery. Herein, we report the discovery of compound 23 (AMG 337), which demonstrates nanomolar inhibition of MET kinase activity, desirable preclinical pharmacokinetics, significant inhibition of MET phosphorylation in mice, and robust tumor growth inhibition in a MET-dependent mouse efficacy model.

Entities:  

Mesh：

Substances：

Year:  2016        PMID： 26812066     DOI： 10.1021/acs.jmedchem.5b01716

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


  8 in total

1.  1,3,4-Oxadiazole and Heteroaromatic-Fused 1,2,4-Triazole Synthesis using Diverted Umpolung Amide Synthesis.

Authors:  Kazuyuki Tokumaru; Kalisankar Bera; Jeffrey N Johnston
Journal:  Synthesis (Stuttg)       Date:  2017-08-07       Impact factor: 3.157

Review 2.  Synthesis and Anticancer Properties of Functionalized 1,6-Naphthyridines.

Authors:  Mallu Lavanya; Chong Lin; Jincheng Mao; Dhakshanamurthy Thirumalai; Sreenath Reddy Aabaka; Xiaojiang Yang; Jinhua Mao; Zhiyu Huang; Jinzhou Zhao
Journal:  Top Curr Chem (Cham)       Date:  2021-02-24

Review 3.  Ockham's razor for the MET-driven invasive growth linking idiopathic pulmonary fibrosis and cancer.

Authors:  Giulia M Stella; Alessandra Gentile; Alice Balderacchi; Federica Meloni; Melissa Milan; Silvia Benvenuti
Journal:  J Transl Med       Date:  2016-09-02       Impact factor: 5.531

4.  MAPK pathway inhibition induces MET and GAB1 levels, priming BRAF mutant melanoma for rescue by hepatocyte growth factor.

Authors:  Sean Caenepeel; Keegan Cooke; Sarah Wadsworth; Guo Huang; Lidia Robert; Blanca Homet Moreno; Giulia Parisi; Elaina Cajulis; Richard Kendall; Pedro Beltran; Antoni Ribas; Angela Coxon; Paul E Hughes
Journal:  Oncotarget       Date:  2017-03-14

5.  Cabozantinib can block growth of neuroendocrine prostate cancer patient-derived xenografts by disrupting tumor vasculature.

Authors:  Mark P Labrecque; Lisha G Brown; Ilsa M Coleman; Holly M Nguyen; Daniel W Lin; Eva Corey; Peter S Nelson; Colm Morrissey
Journal:  PLoS One       Date:  2021-01-20       Impact factor: 3.240

6.  Design, Synthesis, and Biological Evaluation of [1,2,4]triazolo[4,3-a] Pyrazine Derivatives as Novel Dual c-Met/VEGFR-2 Inhibitors.

Authors:  Xiaobo Liu; Yuzhen Li; Qian Zhang; Qingshan Pan; Pengwu Zheng; Xinyang Dai; Zhaoshi Bai; Wufu Zhu
Journal:  Front Chem       Date:  2022-04-06       Impact factor: 5.545

7.  Design, Synthesis, and Evaluation of New Mesenchymal-Epithelial Transition Factor (c-Met) Kinase Inhibitors with Dual Chiral Centers.

Authors:  Han Yao; Yuanyuan Ren; Jun Yan; Jiadai Liu; Jinhui Hu; Ming Yan; Xingshu Li
Journal:  Molecules       Date:  2022-08-23       Impact factor: 4.927

Review 8.  An insight on medicinal attributes of 1,2,4-triazoles.

Authors:  Ranjana Aggarwal; Garima Sumran
Journal:  Eur J Med Chem       Date:  2020-07-27       Impact factor: 6.514
  8 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.