Synthesis And Properties Of Novel Phosphine-Containing Gold(?) Complexes And GSH-Based Fluorescent Probes

Cancer causes one-eighth of all deaths worldwide,and new anti-cancer drugs are urgently needed in the fight against disease.Over the past decade,there has been increasing interest in the development of metal-based complexes for the treatment of cancer.In recent years,gold complexes have received widespread attention as a substitute for platinum drugs in the treatment of cancer.As gold complexes emerge as a substitute for cisplatin,interest in medicinal inorganic chemistry continues to grow.In the first part of the work,five alkynyl gold(I)phosphine complexes Au-1?Au-5 containing polyether chain substitution were designed and synthesized.The in vitro cytotoxicity of these five alkynyl gold(I)phosphine complexes on four tumor cells and two normal cells was studied by MTS method,and a simple antibacterial activity test was carried out.Au-1 was selectively inhibited Hela cells,and showing IC50 equivalent to cisplatin;SA ATCC25923 showed additive effect when Au-1 was combined with vancomycin.Despite important research advances in the field of anticancer inorganic medicinal chemistry,there have been few studies using metal-containing drugs as antibacterial agents.Human society often uses antibacterial agents to treat infections caused by pathogenic microorganisms.Although these antibacterial agents have saved a lot of lives and are an important part of modem medicine,they have led to the evolution of microbial stress and the emergence of resistant mutants.In an emergency,its effectiveness is seriously reduced.Humans have great pain because of their resistance to antibacterial agents,so the need for new effective and non-toxic antibacterial agents is one of the biggest challenges of the 21st century.In the second part of the work,five gold(I)phosphine complexes 3-4a?3-4e containing 5-phenyl-1,3,4-oxadiazole-2-thione were designed and synthesized.The crystal structure of the four complexes was structurally characterized.The in vitro cytotoxicity of these five thiokein gold(I)phosphine complexes on four tumor cells and two normal cells was studied by MTS method,and a simple antibacterial activity test was performed.Among them,3-4c showed good antibacterial properties against Staphylococcus aureus,and the MIC was 3.91?g/mL.Reduced glutathione(GSH)is a thiol-containing tripeptide that is widely present in various biological cells.This specific structure makes it an important antioxidant and free radical scavenger in the body.Given the important role of GSH in cells,how to detect GSH quickly,efficiently,and specifically is very important.Fluorescent probes are widely used in the field of sensing and optical imaging due to their high sensitivity,fast response time and technical simplicity.A fluorescent probe based on GSH detection was also designed and synthesized.In the third part of the work,a fluorescent probe CP based on GSH detection was designed and synthesized.The probe was able to specifically recognize glutathione(GSH)in a PBS buffer solution(pH = 7.4)containing 0.5%(v/v)DMSO.The probe binds to GSH,and the fluorescent color of the probe solution changes from green fluorescence to blue fluorescence after the addition of GSH.The probe can also be successfully applied to Hela cells for in vitro fluorescence imaging.Probe CP is a fluorescent probe that can be successfully used for GSH detection in biological environments.