Quinoline-based promising anticancer and antibacterial agents, and some metabolic enzyme inhibitors

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dc.authoridAhmet Cenk Andaç / 0000-0002-4545-3500en_US
dc.authorscopusidAhmet Cenk Andaç / 20336962400
dc.authorwosidAhmet Cenk Andaç / AAW-5539-2020
dc.contributor.authorÖkten, Salih
dc.contributor.authorAydın, Ali
dc.contributor.authorKoçyiğit, Ümit Muhammet
dc.contributor.authorÇakmak, Osman
dc.contributor.authorErkan, Sultan
dc.contributor.authorAndaç, Ahmet Cenk
dc.contributor.authorTaslimi, Parham
dc.contributor.authorGülçin, İlhami
dc.date.accessioned2020-09-21T12:28:21Z
dc.date.available2020-09-21T12:28:21Z
dc.date.issued2020
dc.departmentİstinye Üniversitesi, Eczacılık Fakültesi, Eczacılık Meslek Bilimleri Bölümüen_US
dc.description.abstractA series of substituted quinolines was screened for their antiproliferative, cytotoxic, antibacterial activities, DNA/protein binding affinity, and anticholinergic properties by using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide cell proliferation, lactate dehydrogenase cytotoxicity, and microdilution assays, the Wolfe–Shimmer equality method, the Ellman method, and the esterase assay, respectively. The results of the cytotoxic and anticancer activities of the compounds displayed that 6-bromotetrahydroquinoline (2), 6,8-dibromotetrahydroquinoline (3), 8-bromo-6-cyanoquinoline (10), 5-bromo-6,8-dimethoxyquinoline (12), the novel N-nitrated 6,8-dimethoxyquinoline (13), and 5,7-dibromo-8-hydroxyquinoline (17) showed a significant antiproliferative potency against the A549, HeLa, HT29, Hep3B, and MCF7 cancer cell lines (IC50 = 2–50 ?g/ml) and low cytotoxicity (?7–35%) as the controls, 5-fluorouracil and cisplatin. The compound–DNA linkages are hyperchromic or hypochromic, causing variations in their spectra. This situation shows that they can be bound to DNA with the groove-binding mode, with Kb value in the range of 2.0 × 103–2.2 × 105 M–1. Studies on human Gram(+) and Gram(?) pathogenic bacteria showed that the substituted quinolines exhibited selective antimicrobial activities with MIC values of 62.50–250 ?g/ml. All tested quinoline derivatives were found to be effective inhibitors of acetylcholinesterase (AChE) and the human carbonic anhydrase I and II isoforms (hCA I and II), with Ki values of 46.04–956.82 nM for hCA I, 54.95–976.93 nM for hCA II, and 5.51–155.22 nM for AChE. As a result, the preliminary data showed that substituted quinolines displayed effective pharmacological features. Molecular docking studies were performed to investigate the binding modes and interaction energies for compounds 2–17 with AChE (PDB ID: 4EY6), hCA I (PDB ID: 1BMZ), and hCA II (PDB ID: 2ABE).en_US
dc.identifier.citationÖkten, S., Aydın, A., Koçyiğit, Ü. M., Çakmak, O., Erkan, S., Andac, C. A., ... & Gülçin, İ. (2020). Quinoline‐based promising anticancer and antibacterial agents, and some metabolic enzyme inhibitors. Archiv der Pharmazie, 353(9), 2000086.en_US
dc.identifier.doi10.1002/ardp.202000086en_US
dc.identifier.issn0365-6233en_US
dc.identifier.issue9en_US
dc.identifier.pmid32537757en_US
dc.identifier.scopus2-s2.0-85090079624en_US
dc.identifier.scopusqualityQ2en_US
dc.identifier.urihttps://doi.org/10.1002/ardp.202000086
dc.identifier.urihttps://hdl.handle.net/20.500.12713/1049
dc.identifier.volume353en_US
dc.identifier.wosWOS:000567558100004en_US
dc.identifier.wosqualityQ2en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.institutionauthorAndaç, Ahmet Cenk
dc.language.isoenen_US
dc.publisherWiley-VCH Verlagen_US
dc.relation.ispartofArchiv der Pharmazieen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectAcetylcholinesterase Enzyme Inhibitionen_US
dc.subjectAntibacterialen_US
dc.subjectAnticancer Activityen_US
dc.subjectCarbonic Anhydrase Enzyme Inhibitionen_US
dc.subjectDNA Bindingen_US
dc.subjectMolecular Dockingen_US
dc.subjectQuinoloneen_US
dc.titleQuinoline-based promising anticancer and antibacterial agents, and some metabolic enzyme inhibitorsen_US
dc.typeArticleen_US

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