Synthesis of selenophene‐based chalcone analogs and assessment of their biological activity as anticancer agents

Selenium is an essential micronutrient that is beneficial to human health. Selenium‐containing drugs have been developed as antioxidants, anti‐inflammatory, and anticancer agents. However, the synthesis of selenium‐containing chalcones has not been fully explored. Therefore, we report the synthesis of novel selenophene‐based chalcone analogs and reveal their biological activities as anticancer agents. Among the seven synthesized molecules, compounds 6, 8, and 10 exhibited anticancer activity with IC50 values of 19.98 ± 3.38, 38.23 ± 3.30, and 46.95 ± 5.68 μM, respectively, against human colorectal adenocarcinoma (HT‐29) cells. Clonogenic assays and Western blot analysis tests further confirmed that compound 6 effectively induced apoptosis in HT‐29 cells through mitochondrial‐ and caspase‐3‐dependent pathways. Novel selenophene‐based chalcone analogs were synthesized and assessed for their biological activities as anticancer agents. Compound 6 showed more potent activity (IC50 = 19.98 ± 3.38 μM) against human colorectal adenocarcinoma cells (HT‐29) than 5‐fluorouracil (IC50 = 41.43 ± 7.90 μM) as a positive control.