Identification of 3-Bromo-1-Ethyl-1H-Indole as a Potent Anticancer Agent with Promising Inhibitory Effects on GST Isozymes
| Autor: | Can Yilmaz, Metin Konus, Sevki Arslan, Abdussamet Kayhan, Aslıhan Kurt-Kızıldoğan, Dogukan Mutlu, Omruye Ozok, Çiğdem Otur, Arif Kivrak |
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| Přispěvatelé: | [Belirlenecek] |
| Rok vydání: | 2021 |
| Předmět: |
Cancer Research
Antifungal Agents Antioxidant Cell Survival medicine.medical_treatment antioxidant activity Antineoplastic Agents Apoptosis Microbial Sensitivity Tests Isozyme Antioxidants Structure-Activity Relationship chemistry.chemical_compound Picrates medicine Humans MTT assay Benzothiazoles Enzyme Inhibitors Cytotoxicity Cells Cultured anti-cancer Cell Proliferation Glutathione Transferase Pharmacology Indole test antimicrobial activity Bacteria Dose-Response Relationship Drug Molecular Structure Biphenyl Compounds Fungi biological activities Glutathione Antimicrobial Anti-Bacterial Agents Isoenzymes chemistry Biochemistry Indole cytotoxicity Molecular Medicine Trolox Drug Screening Assays Antitumor Sulfonic Acids |
| Zdroj: | Anti-Cancer Agents in Medicinal Chemistry. 21:1292-1300 |
| ISSN: | 1871-5206 |
| Popis: | Background: 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. Scientific 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] The 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. WOS:000631838700003 2-s2.0-85103033113 PubMed: 32951581 |
| Databáze: | OpenAIRE |
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