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Exploring the Synergistic Anticancer Potential of Benzofuran-Oxadiazoles and Triazoles: Improved Ultrasound- and Microwave-Assisted Synthesis, Molecular Docking, Hemolytic, Thrombolytic and Anticancer Evaluation of Furan-Based Molecules.

Ali IrfanSadia FaizAzhar RasulRehman ZafarAmeer Fawad ZahoorKatarzyna Kotwica-MojzychMariusz Mojzych
Published in: Molecules (Basel, Switzerland) (2022)
Ultrasound- and microwave-assisted green synthetic strategies were applied to furnish benzofuran-oxadiazole 5a - g and benzofuran-triazole 7a - h derivatives in good to excellent yields (60-96%), in comparison with conventional methods (36-80% yield). These synthesized derivatives were screened for hemolysis, thrombolysis and anticancer therapeutic potential against an A549 lung cancer cell line using an MTT assay. Derivatives 7b (0.1%) and 5e (0.5%) showed the least toxicity against RBCs. Hybrid 7f showed excellent thrombolysis activity (61.4%) when compared against reference ABTS. The highest anticancer activity was displayed by the 5d structural hybridwith cell viability 27.49 ± 1.90 and IC 50 6.3 ± 0.7 μM values, which were considerably lower than the reference drug crizotinib (IC 50 8.54 ± 0.84 μM). Conformational analysis revealed the spatial arrangement of compound 5d , which demonstrated its significant potency in comparison with crizotinib; therefore, scaffold 5d would be a promising anticancer agent on the basis of cytotoxicity studies, as well as in silico modeling studies.
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