The Synthesis and Preliminary Activity Assay In Vitro of Andrographolide Derivatives

Andrographolide, the major labdane diterpenoid from Andrographis paniculata has been reported to be cytotoxic against various cancer cells in vitro. A series of novel andrographolide derivatives were designed and synthesized as antitumor agents. The structures were confirmed by IR, H-1-NMR, and MS. Comparing to andrographolide, most of target compounds showed moderate inhibition activity against human tongue cancer cell line. But all of them displayed low antiproliferative activities. However, 3, 19-cyclophosphate derivatives (7-9) showed relatively high antiproliferative activity, and could be used as lead compounds for exploring new type antitumor agents in the future.