Semisynthesis of new andrographolide derivativeswith cytotoxic activity

Andrographolide is a major metabolite of the ayurvedic medicinal plant of Andrographis paniculata. In an effort to develop potent anti-cancer drugs, a new series of andrographolide derivatives (4a-4e) were designed, synthesized, and evaluated for their cytotoxic activity against lung cancer, leukemia, breast cancer and prostate cancer cell lines. The screening results revealed that the analogues display significant cytotoxic activity against tested cell lines. The dimethylacryloyl derivative 4c had higher activity than parent compound andrographolide1, and standard drug cisplatin against tested cell lines.