Synthesis and Evaluation of Coumarin Metal Complexes for their Potential Activity against Lung Cancer

Abstract

Background: The most prevalent and deadliest cancers around world are lung cancer, primarily due to tobacco
smoking, exposure to radiations, air pollution, and genetic predisposition. The classic compounds available for its
treatment include platinum-based compounds, folic acid analogues, microtubule inhibitors, high molecular weight
monoclonal antibodies, and aromatic heterocycles. However, resistance development, severe toxicity, poor tumor
selectivity, and hypersensitivity reactions account for some of the major drawback of these classes of anti-cancer
drugs. Objectives: Designing safer and novel Schiff base calcium metal complexes of coumarin quantify their
cytotoxic property. Methodology: Five calcium metal complexes of schiff bases of coumarin derivatives were
synthesized and they were screened for their in vitro biological activities. Using methods such as elemental analysis
and spectroscopy, the structures of the synthesized compounds were confirmed. These novel compounds were
evaluated for their antineoplastic potency against the recognized gold standard, cisplatin. The in vitro cytotoxicity
of the complexes against the lung cancer cell line A549 was assessed using the 3-(4,5-dimethylthiazol-2-yl)-2,5-
diphenyltetrazolium bromide test. Results and Conclusion: The metal complex MC1 demonstrated excellent
cytotoxicity on A549, IC50 value of 73.14 μg/mL was seen. Further subjecting this compound to in vivo studies
could lead us to establishing newer anti-cancer agents defying the drawbacks of the existing ones.