Tumor Targeting Macromolecular Imaging Agents And Tumor Targeting Of Macromolecular Anticancer Drugs

Early diagnosis and treatment of malignant tumors is a major problem in the medical field. Cancer is the major diseases that threaten human health. Early diagnosis of cancer patients will greatly improve the therapeutic effect. However, the5-year survival of patients with malignant tumors is very low due to lack of early diagnosis. Early diagnosis and treatment of malignant tumors has become a current research focus of the field of medicine and chemistry.The bottleneck in the diagnosis of cancer is the development of imaging agents. Imaging agent is a radionuclide-labeled drug. Intravenous injection of labeled drugs, the imaging and diagnosis were performed on PET/SPECT (Positron Emission Tomography/Single Photon Emission Computed Tomography). The key issue is the preparation of the carrier agent. We need to find a carrier agent who own low toxic effects to normal tissues and good diagnostic effects. The drug carrier will be accompanied by the bloodstream to various organs, which greatly reduces the concentration in the tumor, then get a bad diagnosis. We need the drug can target to tumor, making the drug carrier own high accumulation in the tumor. The targeted drug’s receptor must be overexpressed in tumor cells. In this article we will preparate the special drug carrier with targeted functionality through linked drugs with targeting function to the drug carrier.Existing anti-cancer drugs are small molecule drugs, so in body metabolism will be very fast, leading to poor treatment. In this article we will connect the anti-cancer drug to the polymeric carrier, greatly extending the residence time of the anti-cancer drugs in tumors. The toxicity of anticancer drugs will be reduced through the polymer carriers, the damage to normal tissue will be cut down.This paper consists of two parts as follow:PartⅠ:IntroductionPart II:Synthesis of the imaging agents. Synthetic drug monomers, diethylene triamine pentacetate acid, D-galactopyranose monomer, D-Galactosamine monomer, chrysin monomer and quercetin monomer were prepared. Diethylene triamine pentacetate acid is a chelating agent of metal radionuclides.HPMAis a skeleton, the other monomers are targeting ligands. These monomers were polymerized to produce tumor targeting imaging agent/drug precursors. The polymer is the tumor diagnostic imaging agent when it chelated the radionuclide. Animal experiments to verify the polymer’s targeting effect. Tumor targeting effect was tested in animal models.Part III:Synthesis of polymer anticancer drugs. The following monomer drugs were prepared:quercetin monomer and5-fluorouracil monomer. The anticancer drug monomers and HPMA were copolymerized to polymer anticancer drugs. The polymer anticancer drugs were obtained by copolymerization of the anticancer drug monomers and HPMA. The anti-cancer results of the polymer anticancer drugs are tested by animal experiments.The structures of all compounds were confirmed by1H-NMR and13C-NMR.