Synthesis of methoxystilbenoid derivatives and evaluation of cytotoxicity against breast cancer cell line

Breast cancer is currently the most common cancer in women. According to the Global Cancer Observatory (Globocan 2020), there are over 2 million new cases of breast cancer diagnosed each year, accounting for 11.7% of all cancers, with an average of approximately 627,000 deaths due to breast cancer annually. Therefore, the search for new drugs that can treat breast cancer with high efficacy and minimal side effects is a pressing issue and is continuously ongoing worldwide. Stilbenoids, natural compounds commonly found in plants, possessed of various biological activities such as antioxidant, anti-inflammatory, antibacterial, and anticancer properties. Literature has shown that derivatives of methoxylated stilbenoids exhibit strong cytotoxic effects against cancer cells due to the presence of methoxy groups on the benzene ring. This paper reports the successful synthesise of 19 stilbenoid derivatives via Wittig coupling reactions between phosphonium ylides and benzaldehyde derivatives. Compounds 9a, 9b and 12 were reported for the first time for their 1H-NMR spectral data. The evaluation of cytotoxic activity against MCF-7 breast cancer cells, at the tested concentration of 100 µg/mL showed that 15/19 derivatives exhibited cytotoxicity I% more than 50%. Among them, compound 2 showed the highest cytotoxicity with I% of 78.33 ± 1.52%, compared to the positive control camptothecin (I% 56.90 ± 0.79).