Study On Synthesis And Character Of Phosphorus Derivatives Of Genistein

Genistein, the simplest of the isoflavonoid compounds of the Leguminosae, is reported to have extensively biological activities, including anti-osteoporosis, anticancery, antibacterial and anti-inflammatory activities. Due to its structural similarity to estradiol, more attention has been paid to its phytoestrogen activities in the past few years. In the work described in the dissertation, the recent studies on pharmacological action, extraction and isolation, pharmacological and structural modifications of genistein were introduced in chapter one.Many biological activities of genistein have made it common interests as mentioned in many published papers. Lots of efforts have been made to synthesized genistein derivetives with better activities in recent years. Structural modification is one of the most important aspects in terms of increasing its water-solubility, lowering its toxicity and improving its biological assimilation. The studies on phosphorus modifications of genistein and non-covalent interactions with a model protein were shown in this dissertation .The relating works included:1.Genistein was modified with five different phosphoryl reagents by Atherton-Todd reaction, and the structures of the new compounds were determined by ESI-MS, NMR and IR, the reaction activities of different phenol- hydroxyl of genistein were discussed.2.Genistein was modified with di-(2-chloroethyl)-phosphoramidic dichloride, and the structure of the new compound was determined by ESI-MS, NMR and IR, furthermore, the data of NMR spectra were assigned completely and analyzed in detail.3.The interactions between the four phosphorlated genistein derivatives and lysozyme were studied, it is found that all the phosphates could form non-covalent complexes with lysozyme.