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

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dc.contributor.authorÖkten, Salih
dc.contributor.authorAydın, Ali
dc.contributor.authorKoçyiğit, Ümit M.
dc.contributor.authorÇakmak, Osman
dc.contributor.authorErkan, Sultan
dc.contributor.authorAndaç, Cenk A.
dc.contributor.authorTaslimi, Parham
dc.date.accessioned2021-01-14T18:10:25Z
dc.date.available2021-01-14T18:10:25Z
dc.date.issued2020
dc.departmentKKÜ
dc.descriptionOkten, Salih/0000-0001-9656-1803; Gulcin, ilhami/0000-0001-5993-1668; aydin, ali/0000-0002-9550-9111; Taslimi, Parham/0000-0002-3171-0633
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 novelN-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 mu g/ml) and low cytotoxicity (similar to 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, withK(b)value in the range of 2.0 x 10(3)-2.2 x 10(5) 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 mu 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), withK(i)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 compounds2-17with AChE (PDB ID: 4EY6), hCA I (PDB ID: 1BMZ), and hCA II (PDB ID: 2ABE).en_US
dc.identifier.citationclosedAccessen_US
dc.identifier.doi10.1002/ardp.202000086
dc.identifier.issn0365-6233
dc.identifier.issn1521-4184
dc.identifier.issue9en_US
dc.identifier.pmid32537757
dc.identifier.scopus2-s2.0-85090079624
dc.identifier.scopusqualityQ1
dc.identifier.urihttps://doi.org/10.1002/ardp.202000086
dc.identifier.urihttps://hdl.handle.net/20.500.12587/12585
dc.identifier.volume353en_US
dc.identifier.wosWOS:000567558100004
dc.identifier.wosqualityQ2
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.indekslendigikaynakPubMed
dc.language.isoen
dc.publisherWILEY-V C H VERLAG GMBHen_US
dc.relation.ispartofARCHIV DER PHARMAZIE
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.typeArticle

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