Solvent free, microwave-assisted synthesis and cytotoxicity evaluation of benzoxazole derivatives

Introduction: This work aims to develop an efficient green synthetic procedure and cytotoxicity evaluation of benzoxazole derivatives, essential building block in medicinal chemistry research owing its broad range pharmacological properties, especially anticancer activity. Methods: The microwave-assisted condensation reaction between 2-amino-4-methylphenol aromatic aldehydes using iodine as the oxidant under solvent-free conditions was explored. prepared benzoxazoles against three human cancer cell lines including Lu-1, Hep-G2 MCF-7 were examined a MTT assay. Results: Five 2,5-disubstituted derivatives have been successfully synthesized good yields (67-90%) microwave irradiation conditions. initial four compounds revealed that 3b 3e exhibited activity (IC50 = 12 μg/mL) 17.9 μg/mL), respectively. Remarkably, compound 3c showed best at IC50 4 μg/mL. Conclusion: Microwave effectively assisted presence facilitate desired total yields. proved be potent candidates for further study development agents.