Synthesis And Antitumor Activity Of Imidazo[1,2-a] Pyridine Compounds

Cancer is the highest mortality rate in the world,About 8.2 million people died of cancer and 14 million new cancer cases in 2012,Latest version of the "World Cancer Report" predicts that global cancer cases will reach 19 million by 2025.Currently,Chemical drug therapy plays an important role in the treatment of cancer,However,Traditional chemotherapeutic drugs limit their application in clinical treatment due to their large dose requirements and strong side effects.In recent years,Domestic and foreign research continues to discover,The receptor tyrosine kinase c-Met is highly expressed and abnormally activated in most cancers and some tumors,It plays a key role in tumor development,invasion and metastasis,and chemotherapy resistance.c-Met,as a key node protein in the tumor signal network pathway,can interact with other kinases and receptors on the cell surface to become a new target for tumor therapy.Small molecule kinase inhibitors have become the most promising class of inhibitors by inhibiting the kinase activity of c-Met,which plays an important role in cancer progression,thereby inhibiting the transduction of intracellular signals and blocking the progression of tumors.Several studies have reported that imidazo[1,2-a]pyridine derivatives have good pharmacological activities such as anticancer,antiviral,antipyretic and analgesic effects.As a kind of molecular structure framework with better biological activity.It makes many drugs containing this fragment have a wide variety of pharmacological activities.Inhibition of c-Met small molecule kinase inhibitor containing imidazo[1,2-a]pyridine as the parent nucleus has not been reported yet.Once successfully developed,it will be a new type of structural anticancer drug.In this paper,2-amino-5-bromopyridine and maleic anhydride are used as the main starting materials to obtain the parent compound by cyclization,chlorination and esterification.On this basis,Modification of functional groups such as hydrolysis reaction,Suzuki reaction,and amidation reaction to the mother nuclear compound.Finally,18 new target compounds containing imidazo[1,2-a]pyridines were obtained,Perform structural characterization confirmation such as hydrogen spectrum and mass spectrometry,And its anti-tumor biological activity was tested...