Synthesis of novel 1, 3, 4-oxadiazole derivatives as anti-esophageal cancer: In-vitro cytotoxic evaluation

Abstract

      In this work, an efficient protocol address a facile procedure employing safer and commercially available starting materials to afford the target products that are 1, 3, 4-oxadiazole derivatives (5a-c) in satisfactory yields with elevated purities. To elucidate these derivatives, their chemical structures were unambiguously confirmed by using different spectroscopic tools including FT-IR, NMR (¹H and ¹³C), Mass spectra, and melting points. The enantiomers of the synthesized derivatives were checked by enantioselective HPLC analysis and NMR study which showed these derivatives obtained as racemates. With the aim to identify in vitro potency of these derivatives, MTT method has been applied to explore and evaluate their antiproliferative efficacy against esophageal cells (SKGT-4). The cell viability testing via MTT assay revealed that these derivatives displayed potent in vitro activity, showing IC₅₀ values with a range of potential inhibition in comparison to the selected drug as a standard reference. The biological activity present in this work showed the synthesized derivatives offer significant antiproliferative efficacy with safer chemotherapeutic leads in medicinal chemistry to explorations for esophageal cancer treatment.