Search results for "EGF-receptor inhibitor"

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Design, Synthesis and Biological Evaluation of Novel Pyrazolo[1,2,4]triazolopyrimidine Derivatives as Potential Anticancer Agents

2021

Three novel pyrazolo-[4,3-e][1,2,4]triazolopyrimidine derivatives (1, 2, and 3) were designed, synthesized, and evaluated for their in vitro biological activity. All three compounds exhibited different levels of cytotoxicity against cervical and breast cancer cell lines. However, compound 1 showed the best antiproliferative activity against all tested tumor cell lines, including HCC1937 and HeLa cells, which express high levels of wild-type epidermal growth factor receptor (EGFR). Western blot analyses demonstrated that compound 1 inhibited the activation of EGFR, protein kinase B (Akt), and extracellular signal-regulated kinase (Erk)1/2 in breast and cervical cancer cells at concentrations…

cervical cancercrystal X-ray analysisPharmaceutical ScienceAntineoplastic AgentsArticleAnalytical ChemistryHeLa03 medical and health sciencesbreast cancerQD241-4410302 clinical medicineDrug DiscoveryHumansEpidermal growth factor receptorPhysical and Theoretical Chemistrypyrazolo[124]triazolopyrimidineCytotoxicityProtein Kinase InhibitorsProtein kinase BCell Proliferation030304 developmental biologyMitogen-Activated Protein Kinase 1pyrazolo[124]triazolopyrimidine; EGF-receptor inhibitor; breast cancer; cervical cancer; molecular docking; crystal X-ray analysis0303 health sciencesBinding SitesMitogen-Activated Protein Kinase 3biologyChemistryKinaseOrganic ChemistryBiological activitymolecular dockingTriazolesbiology.organism_classificationMolecular biologyIn vitroErbB ReceptorsMolecular Docking SimulationPyrimidinesChemistry (miscellaneous)Docking (molecular)030220 oncology & carcinogenesisbiology.proteinMolecular MedicineProto-Oncogene Proteins c-aktEGF-receptor inhibitorHeLa CellsProtein BindingMolecules
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