Abstract: Andrographolide is one of the main active constituent of Andrographis paniculata.Many studies have been done on its structural modification in order to improve the potency.In this paper,a series of andrographolide derivatives with the structure of 12-N-acyl aminomethyl-14-deoxyandrographolide were synthesized starting from the parent compound andrographolide via Michael addition,reduction and amidation reactions.All the compounds were identified by MS and NMR analysis.Their antitumor activities were preliminarily tested on cancer cell lines U87 and MCF-7 by MTT method.However,none of the tested compunds was more potent than the parent compound,suggesting that the long alkyl chains introduced to C-12 of andrographolide might decrease the antitumor activity.