{"title":"Biological evaluation of benzothiazoles obtained by microwave-green synthesis.","authors":"Mesut Ozdincer, Aslihan Dalmaz, Sefa Durmus, Gorkem Dulger, Ilker Kiliccioglu","doi":"10.1590/0001-3765202420230423","DOIUrl":null,"url":null,"abstract":"<p><p>Benzothiazole compounds are known as an important bicyclic ring system with multiple applications. These compounds have a wide range of biological activities, including anticancer, antimicrobial, anti-inflammatory and antiviral activities. In this study, benzothiazole compounds were synthesized and their various biological activities were examined. The synthesized benzothiazoles were evaluated for their antimicrobial properties against various bacterial and fungal strains. The compound 6e is most active ligand in the series against bacteria and fungi as compared to standard antibiotics. Especially, this compound significant effect against Staphylococcus aureus (32.00 ± 1.73 mm). These compounds exhibited potent anticancer activity against gastrointestinal cancer cells, demonstrating their potential as therapeutic agents. The lowest antiproliferative response after administration of the compounds was observed in HCT116 cells, while the most effective antiproliferative response was observed in AGS cells (> 10 µg/mL). In all cell lines, 40 and 100 µg/mL application values of the selected compounds showed significant increases in the expression of caspase-3, 8 and 9. We also utilized a computational docking approach to investigate the interaction of these benzothiazoles with VEGFR-2 kinase. Our docking studies showed that compounds 6a and 6d may be promising therapeutic agents against gastrointestinal system cancers due to their ability to bind to VEGFR-2 kinase.</p>","PeriodicalId":7776,"journal":{"name":"Anais da Academia Brasileira de Ciencias","volume":null,"pages":null},"PeriodicalIF":1.1000,"publicationDate":"2024-07-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Anais da Academia Brasileira de Ciencias","FirstCategoryId":"103","ListUrlMain":"https://doi.org/10.1590/0001-3765202420230423","RegionNum":4,"RegionCategory":"综合性期刊","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2024/1/1 0:00:00","PubModel":"eCollection","JCR":"Q3","JCRName":"MULTIDISCIPLINARY SCIENCES","Score":null,"Total":0}
引用次数: 0
Abstract
Benzothiazole compounds are known as an important bicyclic ring system with multiple applications. These compounds have a wide range of biological activities, including anticancer, antimicrobial, anti-inflammatory and antiviral activities. In this study, benzothiazole compounds were synthesized and their various biological activities were examined. The synthesized benzothiazoles were evaluated for their antimicrobial properties against various bacterial and fungal strains. The compound 6e is most active ligand in the series against bacteria and fungi as compared to standard antibiotics. Especially, this compound significant effect against Staphylococcus aureus (32.00 ± 1.73 mm). These compounds exhibited potent anticancer activity against gastrointestinal cancer cells, demonstrating their potential as therapeutic agents. The lowest antiproliferative response after administration of the compounds was observed in HCT116 cells, while the most effective antiproliferative response was observed in AGS cells (> 10 µg/mL). In all cell lines, 40 and 100 µg/mL application values of the selected compounds showed significant increases in the expression of caspase-3, 8 and 9. We also utilized a computational docking approach to investigate the interaction of these benzothiazoles with VEGFR-2 kinase. Our docking studies showed that compounds 6a and 6d may be promising therapeutic agents against gastrointestinal system cancers due to their ability to bind to VEGFR-2 kinase.
期刊介绍:
The Brazilian Academy of Sciences (BAS) publishes its journal, Annals of the Brazilian Academy of Sciences (AABC, in its Brazilianportuguese acronym ), every 3 months, being the oldest journal in Brazil with conkinuous distribukion, daking back to 1929. This scienkihic journal aims to publish the advances in scienkihic research from both Brazilian and foreigner scienkists, who work in the main research centers in the whole world, always looking for excellence.
Essenkially a mulkidisciplinary journal, the AABC cover, with both reviews and original researches, the diverse areas represented in the Academy, such as Biology, Physics, Biomedical Sciences, Chemistry, Agrarian Sciences, Engineering, Mathemakics, Social, Health and Earth Sciences.