Design,Synthesis And Antitumor Study Of Platinum(Ⅱ),Ruthenium(Ⅱ) And Iridium(Ⅲ)Complexes

The mutation of proto-oncogene will lead to the occurrence of cancer.As the environmental pollution and deterioration of human’s living environment,the incidence of cancer is increasing year by year.Cancer has become a threat to human health.Human beings are also constantly exploring drugs that can inhibit cancer.For the research of anticancer drugs,it is mainly to enable the drug to act on cancer cells,and to inhibit the growth of cancer cells and promote the death of cancer cells.The main mechanisms of inhibiting cancer are interfering with the synthesis of nucleic acids in cancer cells,interfering with the synthesis and function of proteins in cancer cells,embedding DNA in order to interfere with the transcription process,inhibit topoisomerase activity or inhibit specific enzymes and receptors.Cisplatin,carboplatin and oxaliplatin were the early metal drugs used in cancer therapy.These drugs can affect the structure and function of DNA.Based on the application of platinum drugs in anti-tumor,the metal complexes of platinum,ruthenium and iridium with positive charge are used in the preliminary investigation of antitumor activity.The main purpose is that after the complex is introduced into the DNA,the complex specifically recognizes and can intercalate between the base pairs of DNA to interfere with the transcription process or can inhibit the activity of specific enzymes to achieve the purpose of anti-tumor metal complexes can act on specific biological macromolecules,coupled with their good photochemical properties,they can be used as diagnostic reagents.This article is divided into four chapters.The first chapter mainly summarizes the research progress of antineoplastic and metal complexes of platinum,ruthenium and iridium.The second chapter is mainly about the synthesis of 8 platinum complexes and the preliminary exploration of their anti-tumor activity.Among them,the complex P1 exhibits good activity and intercalates with DNA.The complex P3 showed a highly inhibitory activity against T7 RNA polymerase.The third chapter talks about the synthesis and antitumor activity of 8 ruthenium complexes.Among them,the complex[Ru（L4）₂]（PF₆）₂shows a good topoisomerase I inhibitory activity.Chapter 4mainly discusses the synthesis and antitumor activity of 16 iridium complexes.Its antitumor activity is not very prominent,but it shows good activity as a potential sensitizer for two-photon excitation photodynamic therapy.Compounds Y1-Y4 all showed good qualities as two-photon excitation photodynamic therapy reagents and mitochondrial dyes,of which Y3 was the most obvious.