Study Of Synthesis And Antitumor Activity Of Phenylhydronaphthalene

Malignant tumor poses serious threat to people's health, currently among the top causes of death. Prevention and treatment of tumor have been the focus of the field of medicine.Recently, it was an important way that lots of new medicine was found out from several natural products. VBE, the natural products from the seed of Chinese traditional medicine Vitex Negundo with the structure of phenylhydronaphthalene can inhibit the growth of tumor. In preliminary study it was discoveried that the antitumor effects of these compounds was related to the inhibition of PI3K-Akt-mTOR signaling pathway.Because of the difficulty of availability from natural plants and low yield in total synthesis, VBE can be obtained limitedly. In this paper, design, and synthesis of phenylhydronaphthalene analogues was studied and 8 compounds were obtained, of which the structures were confirmed by NMR, IR and MS. The preliminary inhibitory activity assay was carried out in HL-60 leukemia cells with MTT method and A549 lung cancer cells with SRB method. The most potent compound displayed high inhibitory rate of 77.80% in HL-60 cell lines. The preliminary structure-activity relationship of phenylhydronaphthalene derivatives was also studied. The existence of methoxy group on C-7, C-3'position of aromatic ring and hydroxyl group on C-6, C-4'position is more favorable for the inhibitory activity, which can be used to guide the design and synthesis of novel anticancer agent with the structure of phenylhydro naphthalene analogues.