Synthesis Of The Targeted HPMA Copolymer And Highly Branched Polyethylene Carriers

Malignant tumor is a greatly hazardous disease to our health. The most commontherapeutic drugs distribute not only to cancer cells, but also to normal tissue, whichresults in general toxicity and poor acceptance of the treatment by patients. So thetarget delivery of chemotherapeutics to defined cells, either stromal or cancer cells incancer lesions, is one of the main challenges and a very active field of research in thedevelopment of the treatment strategies to improve target and safety of drugs.The key issue is the preparation of the carrier agent. We need to find a carrierwho own low toxic effects to normal tissues and good diagnostic effects. The drugcarrier will be accompanied by the bloodstream to various organs, which greatlyreduces the concentration in the tumor, then get a bad diagnosis. We need the drug cantarget to tumor, making the drug carrier own high accumulation in the tumor. In thisarticle we will preparate the special drug carrier with targeted functionality throughlinked drugs with targeting function to the drug carrier.This paper consists of four chapters as follow:Chapter1: ReviewsChapter2: Synthesis, characterization and in vivo evaluation of tumor targetingN-(2-hydroxypropyl)methacrylamide copolymer conjugates containing sulfamethazi-ne groupswe report the synthesis, characterization and evaluation of a novel sulfameth-azine N-(2-hydroxypropyl)methacrylamide copolymer conjugates for tumor targeting.N-(3-Aminopropyl)methacrylamide-diethylenetriaminepentaacetic acid monomer, m-ethacryloyl-sulfamethazine monomer, poly(N-(2-hydroxypropyl)methacrylamide)-su-lfamethazine-diethylenetriaminepentaacetic acid conjugate, and poly(N-(2-hydroxy-propyl)methacrylamide)-sulfamethazine-diethylenetriaminepentaacetic acid-99mTc we-re successfully synthesized and characterized. Poly(N-(2-hydroxypropyl)methacry-lamide)-diethylenetriaminepentaacetic acid conjugate, diethylenetriaminepentaaceticacid-99mTc and poly(N-(2-hydroxypropyl)methacrylamide)-diethylenetriaminepentaa-cetic acid-99mTc were also synthesized and characterized. Tumor targeting effect wastested in animal models.Chapter3: New ?-diimine nickel(II) complexes containing a Bulky phenethyl substitution: Synthesis, characterization and testing as ethylene polymerizationcatalystsTwo new phenethyl-substituted ?-diimine compounds and their correspondingNi(II) complexes,{bis[N,N?-(2,4/6-dimethylphenyl)imino]acenaphthene}dibromonic-kels were successfully synthesized and characterized by1H NMR,13C NMR, elemen-tal analysis and X-ray crystallography. These complexes activated by aluminium-diethyl chloride (DEAC) were tested in the polymerization of ethylene under mildconditions. The influence of ligand structure and the effects of the Al/Ni molar ratio,polymerization temperature were discussed on the catalyst activity of ethylene poly-merization with DEAC as a co-catalyst. The catalytic activity, polymer molecularweight and polymer degree of branching were significantly affected by the bulkychiral sec-phenethyl substituents in the ortho/para-aryl position. The polymer werecharacterized by1H NMR,13C NMR and gel permeation chromatography (GPC)analysis.Chapter4: Chiral ?-diimine nickel(II) complexes containing bulky sec-phenethylgroups: synthesis, characterization and testing as ethylene polymerization catalystsTwo new phenethyl-substituted ?-diimine compounds and their correspondi-ng Ni(II) complexes,{bis[N,N?-(2,4/6-dimethylphenyl)imino]-2,3-butadiene}dibro-monickels were successfully synthesized and characterized by1H NMR,13C N-MR, elemental analysis and X-ray crystallography. These complexes activatedby aluminiumdiethyl chloride (DEAC) were tested in the polymerization of eth-ylene under mild conditions. The influence of ligand structure and the effectsof the Al/Ni molar ratio, polymerization temperature were discussed on the cat-alyst activity of ethylene polymerization with DEAC as a co-catalyst. The cata-lytic activity, polymer molecular weight and polymer degree of branching weresignificantly affected by the bulky chiral sec-phenethyl substituents in the ort-ho/para-aryl position. The polymer were characterized by1H NMR,13C NMRand gel permeation chromatography (GPC) analysis.