Discovery of [1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives as novel, potent and selective c-Met kinase inhibitors: Synthesis, SAR study, and biological activity.
Sign Up to like & getrecommendations! Published in 2018 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.03.049
Abstract: A series of [1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives were designed, synthesized and evaluated for their biological activity. Most of these compounds showed potent activities against c-Met kinase and cell growth inhibition. The most promising compound, 7d, has the… read more here.
Keywords: biological activity; met kinase; triazolo thiadiazole; thiadiazole derivatives ... See more keywords
Discovery of 1,6-naphthyridinone-based MET kinase inhibitor bearing quinoline moiety as promising antitumor drug candidate.
Sign Up to like & getrecommendations! Published in 2020 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2020.112174
Abstract: A series of 1,6-naphthyridinone-based MET kinase inhibitors bearing quinoline moiety in block A were designed and synthesized based on the structures of Cabozantinib and our reported compound IV. Extensive SAR and DMPK studies led to… read more here.
Keywords: naphthyridinone based; kinase inhibitor; met kinase; based met ... See more keywords
Novel anti-cancer agents based on germacrone: design, synthesis, biological activity, docking studies and MD simulations
Sign Up to like & getrecommendations! Published in 2017 at "RSC Advances"
DOI: 10.1039/c6ra26944c
Abstract: Germacrone is a major activity component found in Curcuma zedoaria oil product, which is extracted from Curcuma zedoaria. In the present study, novel germacrone derivatives were first designed based on the theories of bioalkylating agents,… read more here.
Keywords: docking studies; germacrone; novel anti; met kinase ... See more keywords
Insight into the key features for ligand binding in Y1230 mutated c-Met kinase domain by molecular dynamics simulations
Sign Up to like & getrecommendations! Published in 2018 at "Journal of Biomolecular Structure and Dynamics"
DOI: 10.1080/07391102.2017.1340852
Abstract: c-Met kinase has been considered as an attractive target for developing antitumor agents. The strong interactions between Tyr1230 and the inhibitors emphasized its importance for ligand binding. The clinically related Tyr1230 mutations have made negative… read more here.
Keywords: kinase; kinase domain; ligand binding; met kinase ... See more keywords
Structural Alterations of MET Trigger Response to MET Kinase Inhibition in Lung Adenocarcinoma Patients
Sign Up to like & getrecommendations! Published in 2017 at "Clinical Cancer Research"
DOI: 10.1158/1078-0432.ccr-17-3001
Abstract: Purpose: We sought to investigate the clinical response to MET inhibition in patients diagnosed with structural MET alterations and to characterize their functional relevance in cellular models. Experimental Design: Patients were selected for treatment with… read more here.
Keywords: structural alterations; response; response met; inhibition ... See more keywords
Abstract 1920: Targeting structural RET and MET kinase alterations in lung adenocarcinoma patients
Sign Up to like & getrecommendations! Published in 2018 at "Cancer Research"
DOI: 10.1158/1538-7445.am2018-1920
Abstract: Structural rearrangements that activate receptor kinases account for an ever-increasing pool of druggable targets in lung adenocarcinoma patients. Among these tumors RET kinase fusions and MET alterations represent two genetically distinct groups that share a… read more here.
Keywords: lung adenocarcinoma; kinase; met kinase; adenocarcinoma patients ... See more keywords
Selective MET Kinase Inhibition in MET-Dependent Glioma Models Alters Gene Expression and Induces Tumor Plasticity
Sign Up to like & getrecommendations! Published in 2017 at "Molecular Cancer Research"
DOI: 10.1158/1541-7786.mcr-17-0177
Abstract: The receptor tyrosine kinase (RTK) MET represents a promising tumor target in a subset of glioblastomas. Most RTK inhibitors available in the clinic today, including those inhibiting MET, affect multiple targets simultaneously. Previously, it was… read more here.
Keywords: kinase inhibition; inhibition; selective met; compound ... See more keywords
Design, Synthesis and Biological Evaluation of Novel 4-phenoxypyridine Derivatives Containing Semicarbazones Moiety as Potential c-Met Kinase Inhibitors.
Sign Up to like & getrecommendations! Published in 2020 at "Anti-cancer agents in medicinal chemistry"
DOI: 10.2174/1871520620666200101143307
Abstract: BACKGROUND The Hepatocyte Growth Factor Receptor (HGFR) c-Met is over-expressed and/or mutated in various human tumor types. Dysregulation of c-Met/HGF signaling pathway affects cell proliferation, survival and motility, leading to tumor growth, angiogenesis, and metastasis.… read more here.
Keywords: containing semicarbazones; phenoxypyridine derivatives; derivatives containing; met kinase ... See more keywords