Paeonol And Its Derivatives With Antitumor Activity

Paeonol (2'-hydroxy-4'-methoxyacetophenone) is main component from the root barks of Paeonia Suffru ticcosa Andr and the dried root and the entire plants of Pycnostelma Panicu latum (Bunge)K Schum. It was reported that paeonol has potential anti-atherosclerosis, antibacterial, anti-inflammatory and antitumor activity. Paeonol is an idea lead compound for the stucture modification because its ideal biological activities and simple structure. In this dissertation we made a structural modification of the paeonol. MTT assay showed its structure-activity relationship in the terms of anti-tumor activity. We hoped we would get the better anti-tumor derivatives.At first,we used phenol, resorcinol, phloroglucinol as the starting material,synthesized 31 compounds which include paeonol and its derivatives by the way of acylation, alkylation, reduction.And a compound was first reported.In the second part, we evaluated anti-tumor activity of paeonolLast, we synthesized a series of paeonol's derivatives.Preliminary screening these compounds.Analysised the data and concluded the main results:(1) Paeonol and its derivatives inhibited the growth of Hela and MCF-7 cells in a in a dose-dependent manner.(2) The anticancer pharmacophores of paeonol are 2-and 4-dual-oxygen replacement and ketone carbonyl.4-methoxy structure can enhance paeonol and its derivatives's anti-tumor effect.(3) The anticancer activity of ketone carbonyl side substituents group is in the order:straight-chain alkyl derivatives>benzene derivatives.(4) The more active cytotoxic compounds are 13,27 and 28.In short, we discussed paeonol's inhibition of tumor cell growth in this dissertation through the cell experiment in vitro. Summarized paeonol's structure-activity relationship on antitumor aspects. Synthesised a series of paeonol's derivatives. Got the effective anti-tumor compounds and achieved the desired purpose.