Design, Synthesis And Bioactivity Of 5 - Substituted Dihydrobenzofuran - Imidazolium Salts

Nowadays, cancer ranks second in human disease mortality, which has seriously endangered people’s health. Therefore, the development of new anticancer drugs and clinical application is no doubt an enormous challenge. So far, chemists have isolated and discovered many bioactive natural products. Some of them possessing dihydrobenf-uran and imidazole moieties are confirmed having excellent anti-tumor activity. In this thesis, we designed and synthesized a series of5-subsitituted dihydrobenzofuran-im idazolium salts compounds, and carried on the cytotoxicity screening agaist a panal of tumor cell lines. The purpose was to find novel structure and high selective anti-tumor lead compounds.The thesis consists of two chaprets.In the first chapter, the research progress on biological activity of dihydrobenzofu-ran was briefly reviewed.In the second chapter,26dihydrobenzofuran-imidazolium bromides and17dihy-drobenzofuran-imidazolium chlorides were synthesized and evalvated in vitro agaist a panal of human tumor cell lines.The results showed that most of the imidazolium salts d-isplayed high cytotoxic activity. Compared with commercial anticancer drug (DDP), th-e imidazolium salts have the more powerful antitumor activity.Based on research of this thesis, further modifications and structure-activity relati-ionships can be considered to improved the library of dihydrobenzofuran imidazolium salts compounds, to find the lead compounds with potent antitumor activity.