Design, Synthesis, and Biological Evaluation of Quinoxaline Bearing Tetrahydropyridine Derivatives as Anticancer, Antioxidant, and Anti- Tubercular Agents

Autor: Ganesh, Pavale, Poornima, Acharya, Nilesh, Korgavkar, M M V, Ramana
Rok vydání: 2022
Předmět:
Zdroj: Current Computer-Aided Drug Design. 18:414-424
ISSN: 1573-4099
DOI: 10.2174/1573409918666220804142753
Popis: Background: Quinoxaline and Tetrahydropyridine derivatives showed various biological properties. The combination of these two scaffolds may contribute to good biological activity and may give novel and efficacious bioactive candidates. Objective: The present study aimed to identify bioactive agents with quinoxaline bearing tetrahydropyridine derivatives possessing anticancer, antioxidant, and anti-tubercular agents. Method: A series of novel quinoxaline bearing tetrahydropyridine derivatives have been designed and synthesized in good yields. The synthetic protocol involves three-component Povarov reactions of 6-amino quinoxaline, propenyl guaethol, and substituted aldehydes using BF3·OEt2 as catalyst. The newly synthesized molecules were evaluated for their anticancer activity against four cell lines, i.e. A-549, MCF-7, PC-3, and HepG2. Results: The results from in vitro assay indicated that compound 4a proved to be as potent as the standard drug adriamycin against all cell lines with GI50 values Conclusion: These studies showed that a series of novel quinoxaline bearing tetrahydropyridine derivatives exhibit anticancer, anti-mycobacterial, and antioxidant activities.
Databáze: OpenAIRE