{"title":"Design and Synthesis of Some New Quinoxaline-Thiazole-Benzamide Hybrids: In Vitro Anticancer Activity and Their Molecular Docking Studies","authors":"Gouthami Dasari, Madhuri Pandiri, Vinitha Badithapuram, Rajender Reddy Karnekanti, Jyothi Mandala, Srinivas Bandari","doi":"10.1134/S1068162024060104","DOIUrl":null,"url":null,"abstract":"<p><b>Objective:</b> The quinoxaline compound with molecular formula C<sub>8</sub>H<sub>6</sub>N<sub>2</sub>O, which shows a wide range of biological activities including antiviral, anticancer, antimicrobial, antituberculosis, and antileishmanial. <b>Methods:</b> As a part of our efforts to design new anticancer agents, in this study, we develop quinoxaline-thiazole-benzamide hybrids. The anticancer evolution of these hybrids was studied using the MTT assay method. <b>Results and Discussion:</b> The anticancer activity results exhibit that three compounds, 3,5-dimethoxy-<i>N</i>-(4-(2-oxo-1,2-dihydroquinoxaline-1-carbonyl)thiazol-2-yl)benzamide, 4-methoxy-<i>N-</i>(4-(2-oxo-1,2-dihydroquinoxa line-1-carbonyl)thiazol-2-yl)benzamide, and 3,4-dimethoxy-<i>N</i>-(4-(2-oxo-1,2-dihydroquinoxaline-1-carbonyl)thiazol-2-yl)benzamide were shown remarkable anticancer activity ranging from 1.23 to 1.96 µM, demonstrating greater potency than the standard drug. <b>Conclusions:</b> Finally, the <i>in silico</i> results are strongly supported by <i>in vitro</i> anticancer activity data and tyrosine kinase EGFR inhibitory activity assay results.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"50 6","pages":"2171 - 2181"},"PeriodicalIF":1.1000,"publicationDate":"2024-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Russian Journal of Bioorganic Chemistry","FirstCategoryId":"92","ListUrlMain":"https://link.springer.com/article/10.1134/S1068162024060104","RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"BIOCHEMISTRY & MOLECULAR BIOLOGY","Score":null,"Total":0}
引用次数: 0
Abstract
Objective: The quinoxaline compound with molecular formula C8H6N2O, which shows a wide range of biological activities including antiviral, anticancer, antimicrobial, antituberculosis, and antileishmanial. Methods: As a part of our efforts to design new anticancer agents, in this study, we develop quinoxaline-thiazole-benzamide hybrids. The anticancer evolution of these hybrids was studied using the MTT assay method. Results and Discussion: The anticancer activity results exhibit that three compounds, 3,5-dimethoxy-N-(4-(2-oxo-1,2-dihydroquinoxaline-1-carbonyl)thiazol-2-yl)benzamide, 4-methoxy-N-(4-(2-oxo-1,2-dihydroquinoxa line-1-carbonyl)thiazol-2-yl)benzamide, and 3,4-dimethoxy-N-(4-(2-oxo-1,2-dihydroquinoxaline-1-carbonyl)thiazol-2-yl)benzamide were shown remarkable anticancer activity ranging from 1.23 to 1.96 µM, demonstrating greater potency than the standard drug. Conclusions: Finally, the in silico results are strongly supported by in vitro anticancer activity data and tyrosine kinase EGFR inhibitory activity assay results.
期刊介绍:
Russian Journal of Bioorganic Chemistry publishes reviews and original experimental and theoretical studies on the structure, function, structure–activity relationships, and synthesis of biopolymers, such as proteins, nucleic acids, polysaccharides, mixed biopolymers, and their complexes, and low-molecular-weight biologically active compounds (peptides, sugars, lipids, antibiotics, etc.). The journal also covers selected aspects of neuro- and immunochemistry, biotechnology, and ecology.