Synthesis And Anti-tumor Activities Of Morusignin-L Skeleton Jointed Oxoindole

Morusignin-L（Morusignin-L,2’,4’,5-trihydroxy-3-（γ,γ,γ-hydroxy-dimethyl）propyl-2’’,2"-dimethylpyrano-5",6":6,7-flavonoids）,a HIV-1 5’-LTR sequence（HIV-1 reverse transcriptase promoter）inhibitor,was separated from Morus a Lba L.We implemented the total synthesis of this compound.At the same time,the ske Leton was studied for anti-tumor activity,found that it a Lso has significant anti-cancer activity in vitro.My task is to synthesize a series of derivatives that possess the skeleton of Morusignin-L and the skeleton of Oxoindole,and carries on the research of anti-tumor activity.In this topic,24 derivatives were sysnthesized.The structures were characterized by ¹HNMR,¹³CNMR and HR-ESI-MS.The in vitro anti-tumor activities of derivatives against human leukemia cells（K562）,human prostatic cancer cells（PC-3）and human lung cancer cells（A549）were inverstigated by MTT method.The IC₅₀of DDP for K562,PC-3and A549 were 27.93μmo L/L,25.77μmol/L,29.85μmol/L,respectively.The results showed that the anti-tumor effect of 23derivatives for K562 are same as DDP,5 derivatives have a good activity to PC-3,to A549 have no obvious inhibitory activity.