Design, synthesis and biological evaluation of 6‐substituted quinolines derived from cabozantinib as c‐Met inhibitors
Sign Up to like & getrecommendations! Published in 2019 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.201900101
Abstract: Based on the cabozantinib scaffold, novel c‐Met inhibitors were rationalized from the limited knowledge of structure‐activity relationships for the quinoline 6‐position. Emphasis was given to modifications capable of engaging in additional polar interactions with the… read more here.
Keywords: design synthesis; biological evaluation; met inhibitors; substituted quinolines ... See more keywords
Feed‐forward activation of STAT3 signaling limits the efficacy of c‐Met inhibitors in esophageal squamous cell carcinoma (ESCC) treatment
Sign Up to like & getrecommendations! Published in 2021 at "Molecular Carcinogenesis"
DOI: 10.1002/mc.23306
Abstract: c‐Hepatocyte growth factor receptor (Met) inhibitors have demonstrated clinical benefits in some types of solid tumors. However, the efficacy of c‐Met inhibitors in esophageal squamous cell carcinoma (ESCC) remains unclear. In this study, we discovered… read more here.
Keywords: efficacy met; met inhibitors; stat3; escc ... See more keywords
Synthesis of triazolotriazine derivatives as c-Met inhibitors
Sign Up to like & getrecommendations! Published in 2020 at "Molecular Diversity"
DOI: 10.1007/s11030-020-10067-5
Abstract: Receptor tyrosine kinase c-Met is an important antitumor drug target. Triazolotriazine analogues 2–10 were prepared efficiently and evaluated the enzymatic and cellular c-Met activities. Brief structure–activity relationships of triazolotriazine core and CF2-quinoline part were investigated,… read more here.
Keywords: derivatives met; met inhibitors; synthesis triazolotriazine; triazolotriazine derivatives ... See more keywords
Design, synthesis and antitumor evaluation of novel 5-methylpyrazolo[1,5-a]pyrimidine derivatives as potential c-Met inhibitors.
Sign Up to like & getrecommendations! Published in 2020 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2020.104356
Abstract: A series of novel 5-methylpyrazolo[1,5-a]pyrimidine derivatives (10a-10x) were designed, synthesized, and evaluated for their in vitro inhibitory activities against c-Met kinase and antiproliferative activities against the SH-SY5Y, MDA-MB-231, A549, and HepG2 cell lines. Most of… read more here.
Keywords: methylpyrazolo pyrimidine; novel methylpyrazolo; met inhibitors; pyrimidine derivatives ... See more keywords
Discovery of Potent, Selective Triazolothiadiazole-Containing c-Met Inhibitors.
Sign Up to like & getrecommendations! Published in 2021 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.1c00094
Abstract: Herein, we report a novel series of highly potent and selective triazolothiadiazole c-Met inhibitors. Starting with molecule 5, we have applied structure-based drug design principles to identify the triazolothiadiazole ring system. We successfully replaced the… read more here.
Keywords: potent selective; discovery potent; met inhibitors; triazolothiadiazole containing ... See more keywords
3D-QSAR-aided design of potent c-Met inhibitors using molecular dynamics simulation and binding free energy calculation
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Biomolecular Structure and Dynamics"
DOI: 10.1080/07391102.2018.1479309
Abstract: Abstract Abstract Mesenchymal-epithelial transition factor (c-Met) is a member of receptor tyrosine kinase. It involves in various cellular signaling pathways which includes proliferation, motility, migration, and invasion. Over-expression of c-Met has been reported in various… read more here.
Keywords: molecular dynamics; energy; met inhibitors; dynamics simulation ... See more keywords
Met inhibitors in the treatment of lung cancer: the evidence to date
Sign Up to like & getrecommendations! Published in 2022 at "Expert Opinion on Pharmacotherapy"
DOI: 10.1080/14656566.2022.2062227
Abstract: ABSTRACT Introduction The hepatocyte growth factor (HGF) receptor MET is an oncogenic driver in a subpopulation of Non-small Lung Cancer Cells (NSCLC) at the primary tumor stage or in acquired resistance to treatment with tumor-targeting… read more here.
Keywords: lung cancer; treatment; tumor; met inhibitors ... See more keywords
Recent Advances in the Design and Synthesis of c-Met Inhibitors as Anticancer Agents (2014-Present).
Sign Up to like & getrecommendations! Published in 2017 at "Current medicinal chemistry"
DOI: 10.2174/0929867323666161028161441
Abstract: c-Met, also known as the surface receptor of hepatocyte growth factor receptor (HGFR), is a receptor tyrosine kinase with heterodimer transmembrane. c-Met involves in the activation of several signaling pathways, most of them are implicated… read more here.
Keywords: design synthesis; synthesis met; met inhibitors; recent advances ... See more keywords
In silico Modeling and Toxicity Profiling of a Set of Quinoline Derivatives as c-MET Inhibitors in the treatment of Human Tumors.
Sign Up to like & getrecommendations! Published in 2021 at "Turkish journal of pharmaceutical sciences"
DOI: 10.4274/tjps.galenos.2021.54815
Abstract: Objectives 4-(2-fluorophenoxy) quinoline derivatives constitute one of the chemical classes of hepatocyte growth factor receptor (c-MET) inhibitors, a promising treatment against various human tumors. There are three aims of the present study: (1) To develop… read more here.
Keywords: human tumors; toxicity; developed model; met inhibitors ... See more keywords