Identification of 3-Bromo-1-Ethyl-1H-Indole as a Potent Anticancer Agent with Promising Inhibitory Effects on GST Isozymes

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dc.authoridKIVRAK, Arif / 0000-0003-4770-2686
dc.authoridKONUS, METIN / 0000-0002-9953-1375
dc.authoridMutlu, Dogukan / 0000-0003-3259-5822
dc.authoridOTUR, Cigdem / 0000-0003-3337-7990
dc.authoridYILMAZ, Can / 0000-0002-0028-6614
dc.authoridKURT KIZILDOGAN, ASLIHAN / 0000-0002-9323-0993
dc.authorwosidKIVRAK, Arif / AAQ-8432-2021
dc.authorwosidMutlu, Dogukan / AAL-4976-2021
dc.authorwosidKIVRAK, Arif / W-2196-2017
dc.authorwosidKURT KIZILDOGAN, ASLIHAN / A-1199-2019
dc.contributor.authorYilmaz, Can
dc.contributor.authorArslan, Sevki
dc.contributor.authorMutlu, Dogukan
dc.contributor.authorKonus, Metin
dc.contributor.authorKayhan, Abdussamet
dc.contributor.authorKurt-Kizildogan, Aslihan
dc.contributor.authorKivrak, Arif
dc.date.accessioned2021-11-01T15:05:58Z
dc.date.available2021-11-01T15:05:58Z
dc.date.issued2021
dc.department[Belirlenecek]
dc.description.abstractBackground: Indole-based heterocyclic compounds play important roles in pharmaceutical chemistry due to their unexpected biological and pharmacological properties. Objective: Herein, we describe novel biological properties (antioxidant, antimicrobial and anti-cancer) of 3-bromo-1-ethyl-1H-indole (BEI) structure. Method: BEI was synthesized from 1-Methyl-2-phenylindole and N-bromosuccinimide and was characterized by using 1H and 13C NMR. Cytotoxicity was determined by MTT assay. Apoptosis analysis of BEI was determined by Arthur (TM) image-based Cytometer. Different methods were applied to assess the antioxidant activity of BEI. Molecular docking studies were conducted to determine the interactions of bonding between GST isozymes and BEI. Results: According to the antioxidant and antimicrobial activity assays, BEI compound showed reduced total antioxidant activity compared to the Trolox standard, whereas it showed moderate antimicrobial activity against Aspergillus niger and Phytophora eryhtrospora. Notably, the BEI compound demonstrated substantial selective cytotoxicity for the first time towards cancer cell lines, and there existed a significant decrease in the percentage of live cells treated with BEI, in comparison to the control ones. Interestingly, BEI exhibited a promising glutathione S-transferase isozymes inhibition. Conclusion: The results of this study suggest that BEI seems to be a promising molecule to be used in the design of new anti-cancer agents that provide superiority to present commercial anti-cancer drugs.
dc.description.sponsorshipScientific and Technological Research Council of TurkeyTurkiye Bilimsel ve Teknolojik Arastirma Kurumu (TUBITAK) [115Z020]; Van Yuzuncu Yil UniversityYuzuncu Yil University [FYL-2019-8301, FDP-2018-6862]; Pamukkale UniversityPamukkale University [PAU-BAP-2018-KRM-011]; Samsun Ondokuz Mayis UniversityOndokuz Mayis University [PYO.ZRT.1904.17.053]en_US
dc.description.sponsorshipThe authors thank The Scientific and Technological Research Council of Turkey (Project No: 115Z020), Van Yuzuncu Yil University (FYL-2019-8301 and FDP-2018-6862) Pamukkale University (PAU-BAP-2018-KRM-011) and Samsun Ondokuz Mayis University (PYO.ZRT.1904.17.053) for financial supporting of reactant and reagents.en_US
dc.identifier.doi10.2174/1871520620666200918111940
dc.identifier.endpage1300en_US
dc.identifier.issn1871-5206
dc.identifier.issn1875-5992
dc.identifier.issue6en_US
dc.identifier.pmid32951581
dc.identifier.scopus2-s2.0-85103033113
dc.identifier.scopusqualityQ2
dc.identifier.startpage1292en_US
dc.identifier.urihttps://doi.org/10.2174/1871520620666200918111940
dc.identifier.urihttps://hdl.handle.net/11491/7453
dc.identifier.volume21en_US
dc.identifier.wosWOS:000631838700003
dc.identifier.wosqualityQ3
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.indekslendigikaynakPubMed
dc.institutionauthor[Belirlenecek]
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.subjectIndoleen_US
dc.subjectbiological activitiesen_US
dc.subjectcytotoxicityen_US
dc.subjectantioxidant activityen_US
dc.subjectantimicrobial activityen_US
dc.subjectanti-canceren_US
dc.titleIdentification of 3-Bromo-1-Ethyl-1H-Indole as a Potent Anticancer Agent with Promising Inhibitory Effects on GST Isozymes
dc.typeArticle

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