Synthesis and Determination of Antitumor Activity of Jacaranone and Synthetic Analogs

Natural product jacaranone, 1, and three analog derivatives were synthesized and their apoptotic and necrotic activity against four cancer cell lines was tested. One of these derivatives 7, was more active than the natural product, and exhibited an important necrotic effect against three of the cell lines tested (ovarian carcinoma, liver cancer and breast cancer cells). Derivative 6 was more active than the natural product, and showed a significant apoptotic activity against breast cancer and ovarian carcinoma cells. Some derivatives analyzed in this study showed promising anti-tumor results, nevertheless, further studies have to be done in order to determine their in vivo activity, their mechanism as well as their safety and stability.