Synthesis And Biological Activity Of Flavones

In this thesis, three series of flavones were designed and synthesized, Twelve target compounds including ten unreported compounds were prepared, and the structure of those compounds was confirmed by 1HNMR, ESI-MS and elemental analysis. Finally, we studied their anticancer activity using MTT method.Part 1 IntroductionA introduction of the background, recent study and prospect about flavonoids was made in this part. Our idea about this thesis is also demonstrated briefly. Part 2 Synthesis and Biological Activity of Flavoneamines1. Synthesis of the flavone skeletons2. Synthesis and Biological activity of 8-flavonemethylpolyisoprenyl- aminesSix 8-flavonemethyl-polyisoprenylamines were designed and synthesized. The structures of the target compounds were confirmed by 1HNMR, MS spectra and elemental analysis. All of them, together with the commercial drug melphalan, were tested in vitro for their inhibition on three kinds of cancer cells, K562, CHO and B16. The results demonstrated that the N, N-bis(8-flavonemethyl)geranylamine(17a) possessed better antitumor activity than melphalan. With respect to structural modification of flavones, shorter aliphatic chains were consistently more activating than longer ones. N, N-disubstituted polyisoprenylamines gave better results than N-substituted polyisoprenylamines. 3. Synthesis of PolyaminoflavonesPart 3 Synthesis and Biological Activity of 8-flavonemethyl Nitrogen MustardUsing the 8-methylflavone as the starting material, we synthesized 8-flavonemethyl nitrogen mustard. Its structure was confirmed by 1HNMR, MS spectra and elemental analysis, and its anticancer activity was studied using MTT method. The results demonstrated that the activity of 8-flavonemethyl nitrogen mustard was similar to that of melphalan.