Development of Some Novel Coumarin-Chalcone Compounds as Anti-proliferative Agents

Introduction: Cancer is the world's second leading cause of death and morbidity, behind only heart failure, which claimed the lives of 18.2 million people in 2020. While massive initiatives to establish newer leads and innovative chemotherapeutic methods for combating different types of cancer, continues to be a major concern around the world. As a result, identifying cell-cycle inhibitors and apoptotic triggers to fight cancer cells is an appealing method for finding and developing new anti-tumor drugs.

Materials and Methods: The present study involves the rational development and characterization (both physicochemical and spectroscopy) of coumarin-chalcone compounds (A1–A10) and their anti-proliferative potentials against cancer lines of breast cancer origin (MDA-MB468, MDA-MB231, and MCF-7) and non-cancer breast epithelial cell (184B5).

Results: The compound A2 exhibited the highest anti-proliferative activity against the cell line MDA-MB-231 as indicated by the GI50 value of 10.06 μM, the compound A6 exhibited the highest anti-proliferative activity against the cell line MDA-MB-468 as indicated by the GI50 value of 17.54 μM, the compound A1 exhibited the highest anti-proliferative activity against the cell line MCF-7 as indicated by the GI50 value of 25.86 μM, and the compound A6 exhibited the highest anti-proliferative activity against the cell line 184B5 as indicated by the GI50 value of 23.26 μM.

Conclusion: Furthermore, the research urges medicinal chemists to choose chalcone prototypes with well-defined pathways and SARs while developing more powerful inhibitors. Furthermore, it opens up new pathways for the discovery of anti-cancer derivatives using low molecular weight ligands.