Investigating the Activity of Indole-2-on Derivative Src Kinase Inhibitors Against Chronic Myeloid Leukemia Cells

Basit Öğe Kaydı
dc.authorid0000-0001-6340-5441
dc.authorid0000-0002-2073-1949
dc.authorid0000-0001-8946-7173
dc.contributor.authorCort-Donmez, Aysegul
dc.contributor.authorOlgen, Sureyya
dc.contributor.authorGuner, Ersin
dc.contributor.authorAkgun-Cagliyan, Gulsum
dc.contributor.authorHanikoglu, Ferhat
dc.contributor.authorTunc-Ata, Melek
dc.contributor.authorKilic-Toprak, Emine
dc.date.accessioned2026-01-24T12:29:20Z
dc.date.available2026-01-24T12:29:20Z
dc.date.issued2023
dc.departmentAlanya Alaaddin Keykubat Üniversitesi
dc.description.abstractBackground Src family tyrosine kinases play a potential role in Bcr-Abl-induced leukemogenesis. Src kinase inhibitors are reported as selective inhibitors of chronic myeloid leukemia. Objective Since Src kinase inhibitors have an inhibitive effect on chronic myeloid leukemia, indole derivatives (C-1, C-2, C-3) previously found as potent inhibitors of Src kinase were tested against chronic myeloid leukemia in this study. Methods Cell viability of K562 and R/K562 cells, antiproliferative and antioxidant effects, and inhibition profiles of Bcr-Abl kinase of indole derivatives were determined compared to dasatinib and imatinib. Results The results showed that compounds affected cell proliferation and decreased the levels of Bcr/Abl. These results confirmed that the antileukemic activity of compounds was related to Bcr/Abl expression. Docking studies also presented that compounds are inhibitors of both Src and Abl kinases. Calculation of drug-like properties showed that compounds could be potential drug candidates. Conclusion Among indole-2-on derivatives, previously identified as Src kinase inhibitors, C-2 has been discovered to be a strong anticancer drug that is active against susceptible and resistant K562 cell lines and induces apoptosis.
dc.identifier.doi10.2174/1871520622666220513114205
dc.identifier.endpage122
dc.identifier.issn1871-5206
dc.identifier.issn1875-5992
dc.identifier.issue1
dc.identifier.pmid35570519
dc.identifier.scopus2-s2.0-85144018225
dc.identifier.scopusqualityQ2
dc.identifier.startpage113
dc.identifier.urihttps://doi.org/10.2174/1871520622666220513114205
dc.identifier.urihttps://hdl.handle.net/20.500.12868/5291
dc.identifier.volume23
dc.identifier.wosWOS:000958469200010
dc.identifier.wosqualityQ3
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.indekslendigikaynakPubMed
dc.language.isoen
dc.publisherBentham Science Publ Ltd
dc.relation.ispartofAnti-Cancer Agents in Medicinal Chemistry
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.snmzKA_WoS_20260121
dc.subjectIndole-2-on derivatives
dc.subjectanti-proliferative
dc.subjectcell viability
dc.subjectSrc
dc.subjectABl
dc.subjectdocking
dc.titleInvestigating the Activity of Indole-2-on Derivative Src Kinase Inhibitors Against Chronic Myeloid Leukemia Cells
dc.typeArticle

Dosyalar

Koleksiyon

WoS İndeksli Yayınlar Koleksiyonu
PubMed İndeksli Yayınlar Koleksiyonu
Scopus İndeksli Yayınlar Koleksiyonu