Discovery of new HER2/EGFR dual kinase inhibitors based on the anilinoquinazoline scaffold as potential anti-cancer agents

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dc.AffiliationOctober University for modern sciences and Arts (MSA)
dc.contributor.authorSadek M.M.
dc.contributor.authorSerrya R.A.
dc.contributor.authorKafafy A.-H.N.
dc.contributor.authorAhmed M.
dc.contributor.authorWang F.
dc.contributor.authorAbouzid K.A.M.
dc.contributor.otherDepartment of Pharmaceutical Organic Chemistry
dc.contributor.otherFaculty of Pharmacy
dc.contributor.otherMSA University
dc.contributor.other6th October
dc.contributor.otherCairo
dc.contributor.otherEgypt; Pharmaceutical Chemistry Department
dc.contributor.otherFaculty of Pharmacy
dc.contributor.otherAin Shams University
dc.contributor.otherCairo 11566
dc.contributor.otherEgypt; Pharmaceutical Organic Chemistry Department
dc.contributor.otherFaculty of Pharmacy
dc.contributor.otherAssiut University
dc.contributor.otherAbbassia
dc.contributor.otherCairo
dc.contributor.otherEgypt; Chemistry Laboratory
dc.contributor.otherFaculty of Life and Social Sciences
dc.contributor.otherSwinburne University of Technology
dc.contributor.otherMelbourne
dc.contributor.otherVIC
dc.contributor.otherAustralia
dc.date.accessioned2020-01-09T20:42:18Z
dc.date.available2020-01-09T20:42:18Z
dc.date.issued2014
dc.descriptionScopus
dc.description.abstractHerein, we designed and synthesized certain anilinoquinazoline derivatives bearing bulky arylpyridinyl, arylpropenoyl and arylpyrazolyl moieties at the 4? position of the anilinoquinazoline, as potential dual HER2/EGFR kinase inhibitors. A detailed molecular modeling study was performed by docking the synthesized compounds in the active site of the epidermal growth factor receptor (EGFR). The synthesized compounds were further tested for their inhibitory activity on EGFR and HER2 tyrosine kinases. The aryl 2-imino-1,2-dihydropyridine derivatives 5d and 5e displayed the most potent inhibitory activity on EGFR with IC50 equal to 2.09 and 1.94 ?M, respectively, and with IC50 equal to 3.98 and 1.04 ?M on HER2, respectively. Furthermore, the anti-proliferative activity of these most active compounds on MDA-MB-231 breast cancer cell lines, known to overexpress EGFR, showed an IC50 range of 2.4 and 2.5 ?M, respectively. � 2014 Informa UK Ltd. All rights reserved.en_US
dc.description.urihttps://www.scimagojr.com/journalsearch.php?q=17605&tip=sid&clean=0
dc.identifier.doihttps://doi.org/10.3109/14756366.2013.765417
dc.identifier.doiPubMed ID 23402383
dc.identifier.issn14756366
dc.identifier.otherhttps://doi.org/10.3109/14756366.2013.765417
dc.identifier.otherPubMed ID 23402383
dc.identifier.urihttps://t.ly/zN55V
dc.language.isoEnglishen_US
dc.publisherInforma Healthcareen_US
dc.relation.ispartofseriesJournal of Enzyme Inhibition and Medicinal Chemistry
dc.relation.ispartofseries29
dc.subjectAnilinoquinazolineen_US
dc.subjectEGFRen_US
dc.subjectHER2en_US
dc.subjectKinase inhibitorsen_US
dc.subjectLapatiniben_US
dc.subjectantineoplastic agenten_US
dc.subjectepidermal growth factor receptoren_US
dc.subjectepidermal growth factor receptor 2en_US
dc.subjectmolecular scaffolden_US
dc.subjectphosphotransferase inhibitoren_US
dc.subjectquinazoline derivativeen_US
dc.subjectstaurosporineen_US
dc.subjectantiproliferative activityen_US
dc.subjectarticleen_US
dc.subjectcancer cell cultureen_US
dc.subjectdrug activityen_US
dc.subjectdrug designen_US
dc.subjectdrug synthesisen_US
dc.subjectenzyme inhibitionen_US
dc.subjecthumanen_US
dc.subjectIC 50en_US
dc.subjectmolecular modelen_US
dc.subjectpriority journalen_US
dc.subjectAniline Compoundsen_US
dc.subjectAntineoplastic Agentsen_US
dc.subjectCell Line, Tumoren_US
dc.subjectCell Proliferationen_US
dc.subjectCell Survivalen_US
dc.subjectDrug Discoveryen_US
dc.subjectHumansen_US
dc.subjectMolecular Docking Simulationen_US
dc.subjectMolecular Structureen_US
dc.subjectProtein Kinase Inhibitorsen_US
dc.subjectQuinazolinesen_US
dc.subjectReceptor, Epidermal Growth Factoren_US
dc.subjectReceptor, erbB-2en_US
dc.titleDiscovery of new HER2/EGFR dual kinase inhibitors based on the anilinoquinazoline scaffold as potential anti-cancer agentsen_US
dc.typeArticleen_US
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