Antitumor activity against human promyelocytic leukemia and in silico studies of some benzoxazines

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dc.authoridYildiz, Ilkay/0000-0001-9526-0232
dc.authoridOKSUZOGLU, Emine/0000-0003-4106-1056
dc.authoridYilmaz Ozguven, Serap/0000-0002-6458-2658
dc.authoridYenice Cakmak, Gozde/0000-0002-7632-0997
dc.authorwosidYildiz, Ilkay/A-1851-2016
dc.authorwosidYilmaz Ozguven, Serap/G-1553-2014
dc.contributor.authorOksuzoglu, Emine
dc.contributor.authorYilmaz, Serap
dc.contributor.authorCakmak, Gozde Yenice
dc.contributor.authorAtaei, Sanaz
dc.contributor.authorYildiz, Ilkay
dc.date.accessioned2024-06-12T10:54:23Z
dc.date.available2024-06-12T10:54:23Z
dc.date.issued2023
dc.departmentTrakya Üniversitesien_US
dc.description.abstractCancer is one of the deadliest diseases in the world today, and the incidence of cancer is increasing. Leukemia is a type of blood cancer defined as the uncontrolled proliferation of abnormal leukocytes in the blood and bone marrow. The HL-60 (human promyelocytic leukemia) cell line, derived from a single patient with acute promyelocytic leukemia, provides a unique in vitro model system for studying the cellular and molecular events involved in the proliferation and differentiation of leukemic cells. In this study, antitumor activities on the HL-60 of some of the resynthesized benzoxazine derivatives (BXN-01 and BXN-02) were investigated. The results of in vitro studies obtained were compared a standard drug, etoposide. In vitro results showed that BXN-01 and BXN-02 were found to be extremely effective compared to etoposide (IC50 value: 10 mu M) with IC50 values of 5 nM and 25 nM, respectively. Furthermore, molecular docking studies were carried out for preliminary prediction of possible interaction modes between compounds and the active site of the target macromolecules, hTopo II alpha, HDAC2, and RXRA. Then, in silico ADME/Tox studies were performed to predict drug-likeness and pharmacokinetic properties of BXN-01 and BXN-02. Communicated by Ramaswamy H. Sarmaen_US
dc.identifier.doi10.1080/07391102.2022.2130989
dc.identifier.endpage8190en_US
dc.identifier.issn0739-1102
dc.identifier.issn1538-0254
dc.identifier.issue17en_US
dc.identifier.pmid36300440en_US
dc.identifier.scopus2-s2.0-85140996267en_US
dc.identifier.scopusqualityQ2en_US
dc.identifier.startpage8175en_US
dc.identifier.urihttps://doi.org/10.1080/07391102.2022.2130989
dc.identifier.urihttps://hdl.handle.net/20.500.14551/19034
dc.identifier.volume41en_US
dc.identifier.wosWOS:000874722100001en_US
dc.identifier.wosqualityQ1en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherTaylor & Francis Incen_US
dc.relation.ispartofJournal Of Biomolecular Structure & Dynamicsen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectBenzoxazineen_US
dc.subjectAntitumor Activityen_US
dc.subjectHL-60 Cell Lineen_US
dc.subjectMolecular Dockingen_US
dc.subjectIn Silico ADMETen_US
dc.subjectDna Topoisomerase-Iien_US
dc.subjectAntimicrobial Activityen_US
dc.subjectInhibitorsen_US
dc.subjectEtoposideen_US
dc.subjectAgonistsen_US
dc.subjectPotenten_US
dc.subjectCellsen_US
dc.subjectIdentificationen_US
dc.subjectDerivativesen_US
dc.subjectChallengesen_US
dc.titleAntitumor activity against human promyelocytic leukemia and in silico studies of some benzoxazinesen_US
dc.typeArticleen_US

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