Triazolopyridazine derivatives: Synthesis, cytotoxic evaluation, c-Met kinase activity and molecular docking

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dc.AffiliationOctober University for modern sciences and Arts (MSA)
dc.contributor.authorAhmed E.M.
dc.contributor.authorKhalil N.A.
dc.contributor.authorTaher A.T.
dc.contributor.authorRefaey R.H.
dc.contributor.authorNissan Y.M.
dc.contributor.otherPharmaceutical Organic Chemistry Department
dc.contributor.otherFaculty of Pharmacy
dc.contributor.otherCairo University
dc.contributor.otherCairo
dc.contributor.otherEgypt; Pharmaceutical Organic Chemistry Department
dc.contributor.otherFaculty of Pharmacy
dc.contributor.otherOctober 6 University
dc.contributor.otherGiza
dc.contributor.otherEgypt; Pharmaceutical Chemistry Department
dc.contributor.otherFaculty of Pharmacy
dc.contributor.otherOctober University for Modern Sciences and Arts (MSA)
dc.contributor.otherGiza
dc.contributor.otherEgypt; Pharmaceutical Chemistry Department
dc.contributor.otherFaculty of Pharmacy
dc.contributor.otherCairo University
dc.contributor.otherKasr Elini St.
dc.contributor.otherCairo
dc.contributor.other11562
dc.contributor.otherEgypt
dc.date.accessioned2020-01-09T20:40:31Z
dc.date.available2020-01-09T20:40:31Z
dc.date.issued2019
dc.descriptionScopus
dc.description.abstractNovel series of some triazolo[4,3-b]pyridazine derivatives were designed and synthesized. All the newly synthesized compounds were evaluated for their cytotoxic activity at 10?5 M concentration towards 60 cancer cell lines according to USA NCI protocol. Most of the synthesized compounds showed good activity against SR (leukemia) cell panel. The most active compounds, 2f and 4a were subjected for further evaluation at a five dose level screening and their efficacy for c-Met kinase inhibition was determined in vitro. Binding mode of these derivatives was explored via molecular docking. 2019 Elsevier Inc.en_US
dc.description.urihttps://www.scimagojr.com/journalsearch.php?q=25789&tip=sid&clean=0
dc.identifier.doihttps://doi.org/10.1016/j.bioorg.2019.103272
dc.identifier.doiPubMed ID 31539742
dc.identifier.issn452068
dc.identifier.otherhttps://doi.org/10.1016/j.bioorg.2019.103272
dc.identifier.otherPubMed ID 31539742
dc.identifier.urihttps://t.ly/AXqNp
dc.language.isoEnglishen_US
dc.publisherAcademic Press Inc.en_US
dc.relation.ispartofseriesBioorganic Chemistry
dc.relation.ispartofseries92
dc.subjectc-Met kinaseen_US
dc.subjectCytotoxic activityen_US
dc.subjectPyridazinesen_US
dc.subjectTriazolopyridazinesen_US
dc.subjectcytotoxic agenten_US
dc.subjectphosphotransferase inhibitoren_US
dc.subjectscatter factor receptoren_US
dc.subjecttriazolopyridazine derivativeen_US
dc.subjectantineoplastic activityen_US
dc.subjectArticleen_US
dc.subjectbreast canceren_US
dc.subjectcancer inhibitionen_US
dc.subjectcentral nervous system canceren_US
dc.subjectcolon canceren_US
dc.subjectcontrolled studyen_US
dc.subjectdrug bindingen_US
dc.subjectdrug efficacyen_US
dc.subjectdrug screeningen_US
dc.subjectdrug synthesisen_US
dc.subjectenzyme activityen_US
dc.subjectenzyme inhibitionen_US
dc.subjectGI50en_US
dc.subjecthumanen_US
dc.subjecthuman cellen_US
dc.subjectIC50en_US
dc.subjectin vitro studyen_US
dc.subjectkidney canceren_US
dc.subjectleukemiaen_US
dc.subjectmelanomaen_US
dc.subjectmolecular dockingen_US
dc.subjectnon small cell lung canceren_US
dc.subjectovary canceren_US
dc.subjectpriority journalen_US
dc.subjectprostate canceren_US
dc.subjectproton nuclear magnetic resonanceen_US
dc.subjectstructure activity relationen_US
dc.titleTriazolopyridazine derivatives: Synthesis, cytotoxic evaluation, c-Met kinase activity and molecular dockingen_US
dc.typeArticleen_US
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