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

dc.authorid0000-0003-4106-1056
dc.authorid0000-0002-6458-2658
dc.authorid0000-0002-7632-0997
dc.authorid0000-0002-4752-1968
dc.authorid0000-0001-9526-0232
dc.contributor.authorÖksüzoğlu, Emine
dc.contributor.authorYılmaz, Serap
dc.contributor.authorYenice Çakmak, Gözde
dc.contributor.authorAtaei, Sanaz
dc.contributor.authorYıldız, İlkay
dc.date.accessioned2023-01-16T10:52:31Z
dc.date.available2023-01-16T10:52:31Z
dc.date.issued2023
dc.departmentSabire Yazıcı Fen Edebiyat Fakültesi
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 µM) 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?, 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. Sarma.
dc.identifier.doi10.1080/07391102.2022.2130989
dc.identifier.issn0739-1102
dc.identifier.pmid36300440
dc.identifier.scopusqualityQ1
dc.identifier.urihttps:/dx.doi.org/10.1080/07391102.2022.2130989
dc.identifier.urihttps://hdl.handle.net/20.500.12451/9938
dc.identifier.wosWOS:000874722100001
dc.identifier.wosqualityQ1
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.indekslendigikaynakPubMed
dc.language.isoen
dc.publisherTaylor and Francis Ltd.
dc.relation.ispartofJournal of Biomolecular Structure and Dynamics
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/embargoedAccess
dc.subjectAntitumor Activity
dc.subjectBenzoxazine
dc.subjectHL-60 Cell Line
dc.subjectIn Silico ADMET
dc.subjectMolecular Docking
dc.titleAntitumor activity against human promyelocytic leukemia and in silico studies of some benzoxazines
dc.typeArticle

Dosyalar

Orijinal paket
Listeleniyor 1 - 1 / 1
[ X ]
İsim:
oksuzoglu-emine-2022.pdf
Boyut:
4.75 MB
Biçim:
Adobe Portable Document Format
Açıklama:
Tam Metin / Full Text
Lisans paketi
Listeleniyor 1 - 1 / 1
[ X ]
İsim:
license.txt
Boyut:
1.44 KB
Biçim:
Item-specific license agreed upon to submission
Açıklama: