Biochemical Activity of Chalcone Derivatives as Target-Oriented Anti-cancer Agents

Cancer remains a major health burden globally, characterized by uncontrolled cell growth, resistance to therapy, and adverse side effects from current treatments such as chemotherapy. Chalcones, naturally derived phytochemicals, present a promising avenue for anticancer therapy due to their affordability, availability, and low toxicity. This study evaluates the anticancer efficacy of novel polymethylated chalcone derivatives synthesized via reactions involving 2,3,5,6-tetramethylbenzaldehyde and acetophenone. The chalcones were tested against human cancer cell lines and in vivo models, comparing their effects to the standard chemotherapy drug 5-fluorouracil (5-FU). The synthesized compounds demonstrated significant antiproliferative activity, induced apoptosis, and caused G2/M cell cycle arrest. In vivo studies showed reduced tumor size, improved survival rates, and minimal adverse effects on liver and kidney functions compared to 5-FU. These findings underscore the potential of polymethylated chalcone derivatives as targeted anticancer agents, paving the way for further studies and potential clinical applications. s . s. s. s.