Design And Preparation Process Of Transition Metal Ruthenium（Ⅱ） Complex And Iridium（Ⅲ） Complex Anti-Tumor Drugs

Cancer is a disease characterized by uncontrolled cell growth,which has been one of the leading causes of death in the world in the past decades,and the second leading cause of death in the United States after heart related diseases.Despite its success and high cure rate,But there is a dose limitation for cisplatin.side effects and tumor resistance.Ruthenium complexes are promising anticancer agents due to their low toxicity and antitumor efficacy.Photodynamic therapy（PDT）is a clinically non-invasive method of cancer phototherapy,which uses photosensitizer（PS）and light to convert molecular oxygen into highly active and destructive reactive oxygen species（ROS）.In the field of anticancer compounds,ruthenium（II）polypyridyl complexes have been widely recognized because of their antitumor properties.The ruthenium（II）therapeutic agent TLD1433 based on photodynamic therapy has also entered clinical trials.Therefore,ruthenium（II）polypyridine has been proved to be an effective new,alternative and non-invasive photosensitizer for tumor therapy.Iridium（Ⅲ）complexes with cyclic metallization have abundant photophysical properties and can be designed as organelle targeting agents for photodynamic therapy.The strength of interaction between the complex and DNA and the ability to produce singlet oxygen are the preliminary exploration to reflect its anti-tumor activity.Most metal complexes can inhibit the growth of tumor cells by inserting DNA base pairs and acting as to enzyme inhibitors to inhibit DNA replication and transcription.Metal complexes photosensitizers can produce reactive oxygen species to destroy tumor cells under near infrared/visible light.In this paper,the interaction ability and PDT effect of transition metal ruthenium（II）and iridium（III）complexes with DNA were studied.The aim of this study was to study the way of their interaction with DNA to achieve antitumor,the ability to inhibit topoisomerase activity,hydrophilicity and lipophilicity,and the ability to produce singlet oxygen.This paper is divided into four chapters.The first chapter mainly introduces the research progress and activity of transition metal complexes.In Chapter 2,the synthesis,spectroscopic and electrochemical properties of the complexes were studied.Thirteen ruthenium polypyridyl complexes and four iridium complexes were synthesized and studied.In the third chapter,the interaction between complexes and DNA is discussed,including the way of interaction and binding ability.In the fourth chapter,the PDT effect of the complexes was studied.The lipophilic and hydrophilic abilities of the complexes were determined by the determination of oil-water partition coefficient,and the ability and rate of producing singlet oxygen were also determined.Most complexes showed good PDT effect.