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Published on: March 31, 2021
Oxazole-4,5-dicarboxylate derivatives as multifunctional targets against oral cancer and Streptococcus mutans oral
Tamilvelan Manjunathan1, Ajay Guru2
1Department of Chemistry, Faculty of Engineering and Technology, Jain University, Bangalore, India.
Aims:
A mild and metal free method was employed for the synthesis of various substituted oxazoles (C1-C5). These compounds demonstrated the ability to quench ROS in an in vitro antioxidant assay. The biological studies were further expanded to evaluate the properties of these oxazole derivatives against oral pathogens and oral squamous cell carcinoma.
Materials And Methods:
The antimicrobial activity was investigated against Streptococcus mutans oral pathogens using zone of inhibition and MIC assays. The interaction of the derivatives with the Antigen I/II carboxy-terminus receptor of S. mutans was studied. For anticancer studies, cytotoxic effects were evaluated. Network pharmacology experiments were conducted to identify the targets of C5 against oral cancer and gene expression analysis was performed.
Results:
Among the derivatives, C5 exhibited superior antimicrobial activity against S. mutans. The oxazole derivatives showed cytotoxic effects on oral squamous cell carcinoma. Gene expression analysis revealed that C5 enhanced the upregulation of Caspase-3, Caspase-8, and FasL.
Conclusions:
These findings emphasize that among the synthesized oxazole derivatives, C5 has better potential on promoting oral health through its antimicrobial and anticancer activities.
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