Design,Synthesis And Biological Activity Research Of A Targeted Small Molecule Compounds

Tyrosine kinase over-expression can lead to tumors,abnormal activity of them can be used to diagnose cancer in many cases.This paper is on the basis of the ARRY-334543' basic structure and the relationship of quinazoline compound and Efficacy,we obtained above compounds with anti-tumor cell activity by structural modification.These compounds and ARRY-334543 are all belong to the family of tyrosine kinase inhibitor compound,they take the epidermal growth factor receptor tyrosine kinase on(ErbB-1)and ErbB-2(HER-2)as targets.Thereby,they can inhibite activity of tyrosine kinase to treatl cancer.We firstly introduced at the 4,position of 4-amino quinazoline compounds on deacetylase inhibitor Histone hydroxamic acid fragment.We also replaced ether structure by amine structure at 4 'position of quinazoline compounds.We also connected compounds which having an ester group or a straight-chain alkanes at this site.We also directly substituted 4,site of quinazoline by compound N-(5-amino-2-methylphenyl)-4-(3-pyridyl)-2-amino-pyrimidine compound to obtain a new compound.The paper take 4-chloro-6,7-dimethoxy quinazoline,4-chloro-6,7-bis(methoxyethoxy)quinazoline,ethyl bromoacetate,ethyl 8-bromo-octanoic acid acrylate,n-butylbromide and other synthesized a series of compoundsas raw material in this papers.These compounds were characterized by NMR,MS and Infrared confirmed structure of these compounds.Finally,the compounds which we had synthesized were tests to get the result of anti-tumor cell activity,active values of these compounds has basically reached the expected,it indicates that they have certain degree of inhibition against tumor cells.