The Anticancer Potentials of Substituted Indeno[1,2-b]quinoline Amines against HT29 and SW620: Experimental and In silico Approach

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dc.authoridaydin, ali/0000-0002-9550-9111
dc.authoridTutar, Ahmet/0000-0001-5524-8001
dc.authoridOkten, Salih/0000-0001-9656-1803
dc.contributor.authorOkten, Salih
dc.contributor.authorAydin, Ali
dc.contributor.authorErkan, Sultan
dc.contributor.authorTutar, Ahmet
dc.date.accessioned2024-10-26T18:09:39Z
dc.date.available2024-10-26T18:09:39Z
dc.date.issued2024
dc.departmentSivas Cumhuriyet Üniversitesi
dc.description.abstractBackground: This study aimed the determination of the antiproliferative and cytotoxic activities of recently prepared indeno [1,2-b]quinoline amines against colon carcinoma, HT29 and SW620 cell lines by using cell proliferation and cytotoxicity assays.Methods: In vitro inhibition of cell proliferation of indenoquinoline derivatives was determined with an MTT cell proliferation assay. On the other hand, their cell cytotoxicities and apoptotic potential were investigated by LDH cytotoxicity and DNA laddering assays. Moreover, molecular docking studies were performed between the compounds and PDB ID: 1OLG and 4LVT target proteins using virtual scanning techniques.Results: Most of the compounds (1, 3, and 7-9) exhibit much more potent antiproliferative activity than positive controls against HT29 and SW620 cell lines (IC50 values 1.1 - 4.1 mu g/mL) and show slightly toxic properties (percent cytotoxicity 9.8% to 33.5%) to cells compared to positive control. On the other hand, it was determined that effective compounds 1, 2, 3 and 9 stimulated apoptosis on HT29 and SW620. Moreover, the anticancer effect of the recent indeno[1,2-b]quinoline amine derivatives was investigated with the help of molecular docking simulations for their pharmacokinetics. The molecular docking results displayed that mono bromo (1-3) and phenyl (7-9) substituted indeno [1,2-b]quinoline amines interact with mutated p53 and protein Blc-2 residues with hydrogen bonding and polar interactions, respectively.Conclusion: As a result, the preliminary experimental data and in silico studies indicated that the monosubstituted indenoquinoline amine derivatives, especially 1, 3, and 7-9, exhibit effective pharmacological properties.
dc.identifier.doi10.2174/1570180820666230201144615
dc.identifier.endpage151
dc.identifier.issn1570-1808
dc.identifier.issn1875-628X
dc.identifier.issue1
dc.identifier.scopus2-s2.0-85178273018
dc.identifier.scopusqualityQ3
dc.identifier.startpage143
dc.identifier.urihttps://doi.org/10.2174/1570180820666230201144615
dc.identifier.urihttps://hdl.handle.net/20.500.12418/30208
dc.identifier.volume21
dc.identifier.wosWOS:001134916100016
dc.identifier.wosqualityN/A
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.language.isoen
dc.publisherBentham Science Publ Ltd
dc.relation.ispartofLetters in Drug Design & Discovery
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.subjectIndenoquinoline amine
dc.subjectanticancer activity
dc.subjectHT29
dc.subjectSW620
dc.subjectmolecular docking
dc.subjectapoptosis
dc.titleThe Anticancer Potentials of Substituted Indeno[1,2-b]quinoline Amines against HT29 and SW620: Experimental and In silico Approach
dc.typeArticle

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