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Analysis of quinolinequinone analogs with promising cytotoxic activity against breast cancer

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dc.contributor.authorYILMAZ GÖLER, AYŞE MİNE
dc.contributor.authorsYILMAZ GÖLER A. M., Tarbin Jannuzzi A., Biswas A., Mondal S., Basavanakatti V. N., Jayaprakash Venkatesan R., YILDIRIM H., Yıldız M., ÇELİK ONAR H., BAYRAK N., et al.
dc.date.accessioned2023-09-13T11:59:15Z
dc.date.available2023-09-13T11:59:15Z
dc.date.issued2023-01-01
dc.description.abstractIt is quite challenging to find out bioactive molecules in the vast chemical universe. Quinone moiety is a unique structure with a variety of biological properties, particularly in the treatment of cancer. In an effort to develop potent and secure antiproliferative lead compounds, five quinolinequinones (AQQ1-5) described previously have been selected and submitted to the National Cancer Institute (NCI) of Bethesda to envisage their antiproliferative profile based on the NCI Developmental Therapeutics Program. According to the preliminary in vitro single-dose anticancer screening, four of five quinolinequinones (AQQ2-5) were selected for five-dose screening and they displayed promising antiproliferative effects against several cancer types. All AQQs showed a excellent anticancer profile with low micromolar GI50 and TGI values against all leukemia cell lines, some non-small cell lung and ovarian cancer, most colon, melanoma, and renal cancer, and in addition to some breast cancer cell lines. AQQ2-5 reduced the proliferation of all leukemia cell lines at a single dose and five additional doses, as well as some non-small cell lung and ovarian cancer, the majority of colon cancer, melanoma and renal cancer, and some breast cancer cell lines. This motivated us to use in vitro, in silico, and in vivo technologies to further investigate their mode of action. We investigated the in vitro cytotoxic activities of the most promising compounds, AQQ2 and AQQ3, in HCT-116 colon cancer, MCF7 and T-47D breast cancer, and DU-145 prostate cancer cell lines, and HaCaT human keratinocytes. Concomitantly, IC50 values of AQQ2 and AAQ3 against MCF7 and T-47D cell lines of breast cancer, DU-145 cell lines of prostate cancer, HCT-116 cell lines of colon cancer, and HaCaT human keratinocytes were determined. AQQ2 exhibited anticancer activity through the induction of apoptosis and caused alterations in the cell cycle. In silico pharmacokinetic studies of all analogs have been carried out against ATR, CHK1, WEE1, CDK1, and CDK2. In addition to this, in vitro ADME and in vivo pharmacokinetic profiling for the most effective AAQ (AAQ2) have been studied.
dc.identifier.citationYILMAZ GÖLER A. M., Tarbin Jannuzzi A., Biswas A., Mondal S., Basavanakatti V. N., Jayaprakash Venkatesan R., YILDIRIM H., Yıldız M., ÇELİK ONAR H., BAYRAK N., et al., "Analysis of Quinolinequinone Analogs with Promising Cytotoxic Activity against Breast Cancer", Chemistry and Biodiversity, 2023
dc.identifier.doi10.1002/cbdv.202300848
dc.identifier.issn1612-1872
dc.identifier.urihttps://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=85168585991&origin=inward
dc.identifier.urihttps://hdl.handle.net/11424/293404
dc.language.isoeng
dc.relation.ispartofChemistry and Biodiversity
dc.rightsinfo:eu-repo/semantics/openAccess
dc.subjectBiyomedikal Mühendisliği
dc.subjectYaşam Bilimleri
dc.subjectBiyoteknoloji
dc.subjectMoleküler Biyoloji ve Genetik
dc.subjectSitogenetik
dc.subjectKimya
dc.subjectTemel Bilimler
dc.subjectMühendislik ve Teknoloji
dc.subjectBiomedical Engineering
dc.subjectLife Sciences
dc.subjectBiotechnology
dc.subjectMolecular Biology and Genetics
dc.subjectCytogenetic
dc.subjectChemistry
dc.subjectNatural Sciences
dc.subjectEngineering and Technology
dc.subjectMühendislik, Bilişim ve Teknoloji (ENG)
dc.subjectTemel Bilimler (SCI)
dc.subjectYaşam Bilimleri (LIFE)
dc.subjectMühendislik
dc.subjectMikrobiyoloji
dc.subjectBİYOKİMYA VE MOLEKÜLER BİYOLOJİ
dc.subjectBİYOTEKNOLOJİ VE UYGULAMALI MİKROBİYOLOJİ
dc.subjectMÜHENDİSLİK, BİYOMEDİKAL
dc.subjectEngineering, Computing & Technology (ENG)
dc.subjectNatural Sciences (SCI)
dc.subjectLife Sciences (LIFE)
dc.subjectENGINEERING
dc.subjectCHEMISTRY
dc.subjectMOLECULAR BIOLOGY & GENETICS
dc.subjectMICROBIOLOGY
dc.subjectBIOCHEMISTRY & MOLECULAR BIOLOGY
dc.subjectBIOTECHNOLOGY & APPLIED MICROBIOLOGY
dc.subjectENGINEERING, BIOMEDICAL
dc.subjectBiyomühendislik
dc.subjectFizik Bilimleri
dc.subjectBiyokimya
dc.subjectGenel Kimya
dc.subjectMoleküler Tıp
dc.subjectMoleküler Biyoloji
dc.subjectBioengineering
dc.subjectPhysical Sciences
dc.subjectBiochemistry
dc.subjectGeneral Chemistry
dc.subjectMolecular Medicine
dc.subjectMolecular Biology
dc.subjectADME
dc.subjectbreast cancer
dc.subjectcytotoxicity
dc.subjectmolecular docking
dc.titleAnalysis of quinolinequinone analogs with promising cytotoxic activity against breast cancer
dc.typearticle
dspace.entity.typePublication
local.avesis.id90788ac2-e1ea-4a0b-b324-a77676cba67f
local.indexed.atPUBMED
local.indexed.atSCOPUS
local.indexed.atWOS
relation.isAuthorOfPublication8a72311b-9078-47c0-9fd8-bd73292b7739
relation.isAuthorOfPublication.latestForDiscovery8a72311b-9078-47c0-9fd8-bd73292b7739

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