Synthesis and Anticancer Evaluation of Some Glycine Conjugated Hybrid Compounds Containing Coumarin, Thiophene and Quinazoline Moieties

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Abstract

Background/Objectives: Cancer is one of the leading causes of death worldwide, so that 10 million people died from cancer worldwide in 2020. Among them, prostate and breast cancer are the most frequently diagnosed cancer in the world. Methods: Nota-bly, compound 9f displayed the highest activity against both Prostate cancer (PC-3) and Breast cancer (MCF-7) cell lines. It was seen that substitution on the coumarin ring had a positive effect on anticancer activity (exept chlorine substitution on 6th position of coumarin), while it had a negative effect on the selectivity index (the ratio of IC50 cal-culated for healthy and cancer cells). Conclusions: The findings are consistent with the results obtained in the Molecular Docking results. Molecular docking studies were performed to investigate the binding affinities of the synthesized compounds towards kinesin-associated motor protein EG5, Human Ribonucleotide Reductase and Human Topoisomerase II, confirming their potent in vitro cytotoxicity against cancer cell lines. In accordance with the findings of experimental studies, compound 9f demonstrated the optimal docking binding scores.

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