Newer tetrahydropyridine chalcones were synthesized and tested for their antioxidant and anticancer activity. These molecules showed significant anticancer activity at IC50 < 50 μM in human cancer cell lines such as A549 (lung adenocarcinoma), HepG2 (hepatocellular liver carcinoma), HeLa (cervical cancer), HCT-116 (colon carcinoma cells), MCF-7 (breast cancer cell line), and MDA MB 231 (breast cancer cells) cancer cells. The test compounds significantly inhibited cancer cell migrations in scratch wound assay for angiogenesis. Further, the test compounds bearing naphthalene substituents on the main ring showed in vitro antioxidant activity at <100 μM by 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical cation, superoxide radical scavenging, O-phenonthroline, and lipid peroxidation assays. In conclusion, two test compounds bearing naphthalene substitutions exhibited potent anticancer activity that could be attributed to their ability to induce apoptosis, inhibit cancer cell migrations, provide anti-angiogenic properties, and also partly by reducing oxidative stress by scavenging free radicals.
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