| abstract |
The present invention discloses a class of phenylallyl cyclohexenone derivatives with nthe general structure shown in general formula I: n0 n5 R nI nThe present invention combines the structural characteristics and structure-activity nrelationships of piperlongumine, replacing the amide bond with a double bond, while nretaining the active group, changing the aromatic ring substituents, so as to design a n10 novel type of phenylallyl cyclohexenone derivatives targeting the highly expressed nthioredoxin reductase (TrxR) in tumor tissues. It overcomes the shortcomings of nmultiple synthesis steps and expensive metal catalysts for the preparation of npiperlongumine, and improves the anti-tumor activity of piperlongumine. These nresearch results show that the compounds of the present invention have strong n15 inhibitory effects on the proliferation in many tumor cells, and can significantly nincrease the level of ROS in tumor cells to enhance their antitumor effects. |