Abstract

Andrographolide is a labdane diterpenoid from Andrographis paniculata and has been used in the clinic for several decades to treat a variety of diseases in east Asia. In the present study, modification of 12-thioether andrographolide was carried out to seek compounds with better antitumor activity and drug-like properties. A series of novel 3,19-modified thioether andrographolide derivatives were synthesized and evaluated for their in vitro anticancer activities against human breast cancer cells. The results are promising and important in the further development of anticancer agents.

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