Synthesis And Characterization Of A Series Of Anticancer Sulfadiazine Drugs

Chemical therapy is a method which is commonly used in the clinical treatment of cancer by chemical drugs. However, as many drugs for other diseases, the most chemical therapy drugs are not specific, and can also kill the normal cells. So researches on looking for the new medical compounds with higher activities and fewer side effects are the main task in medical chemistry field.In modern medical chemistry, people usually try to design a series of compounds with potential drug activities and biological activities but without toxicological properties. The synthesis and research are based on the purposes improving the activities of the drugs or decreasing the side effects. In the study, a number of functional groups with high activities are interested, such as sulfonamide group, pyrimidinyl group and so on.In this work, we designed two core compounds which have sulfonamide group and pyrimidinyl group in the nucleus chain. In addition, we designed some side chains which were connected with the core compounds and the target compounds were obtained, which have potential drug activities.Firstly, two core compounds,4-(4-bromopyrimidin-2-ylamino)-N-(3-diethyl-aminopropyl)benzenesulfonamide and 4-(4-bromopyrimidin-2-ylamino)-N-(3--dimethylaminopropyl)benzenesulfonamide were synthesized. Secondly, several side chains were synthesized, such as 7-(4,4,5,5-tetramethyl-[l,3,2]-dioxaborolan-2-yl)-1-H-indazole, 1-H-indol-5-ylamine,4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-phenol, isoquinolin-6-ylamine and so on. Finally, the target products were synthesized with the core compounds and the side chains by Suzuki reaction or Buchwald reaction.In the work, all of the synthesized compounds were characterized by 1HNMR, LC-MS and so on.