Abstract: The objectives of this study were to synthesize bis(3-morpholinopropoxy)curcumin (PR1) and to evaluate its antitumor activity.PR1 was synthesized from curcumin and  N-(3-chloropropyl) morpholine.The in vitro antitumor activities of PR1 was evaluated through MTT assays against gastric carcinoma cells (OS-RC-2 and 786-O) and chronic myelogenous leukemia resistance cell (KA).The in vivo antitumor activities of PR1 were evaluated by its growth inhibition of human colon cancer HT29 tumor xenograft in BALB/C-nu nude mice.Compared with curcumin,PR1 showed improved activities against OS-RC-2, 786-O cells,while less activities against KA cell.PR1 showed remarkable in vivo tumor growth inhibition activity.A dose of 100 mg/kg·d was able to inhibit the growth of HT29 xenograft in BALB/Cnu nude mice by 55.7%.No obvious decrease on the body weight of tested nude mice was observed.In conclusion,PR1 showed obvious antitumor activities both in vitro and in vivo.

Key words: curcumin, curcumin derivatives, bis(3-morpholinopropoxy)curcumin, antitumor activity