Studies On The Synthesis, Anti-tumour Activities And The Reactivity Of The Cis-aurated Complexexes With Pyrazole And Its Derivatives

In order to prepare new compounds for the screening of anti-tumor medicine, we changed the structure of the cycloaurated complexes by the modification of the first ligand and the second ligand.After the cycloaurated complexes AuCl₂L¹ which was synthesized by using the protecting group of 2-phenylpyridine have been obtained, we studied the reactivity, with pyrazole and derivatives reactant. The differences of the steric hindrance which results from the substituents on the ring of the pyrazole led to distinctive products, one is mononuclear, and another is dinuclear, both of their crystal structures were determined.As the cycloauration with the protecting group of 5-Methyl-2-phenoxypyridine has been carried out, we got the complexes AuCl₂L², and determined its crystal structure. Then we did the same reactions as we studied on the complexes AuCl₂L¹, but the results were quite different. Two kinds of crystal have been obtained in the same pot. Based on X-ray analysis, both of them were trinuclear complexes; one has three Au(I) atoms, and the other one has two Au(I) atoms and one Au(III) atom.We compared with the chemical construction of the two kinds of cycloaurated compounds after the crystal structures were determined. Au atom in the molecular AuCl₂L² formed a six member ring whose satiric hindrance was much bigger than that of five member AuCl₂L¹, the coordination plan of Au-Cl-Cl-C-N was twisted. Moreover, the bond lengthes of Au-N and Au-C was elongated a little. These factors explained why the AuCl₂L² is not stable as AuCl₂L¹ when reacted with pyrazoles.In addition, we checked the anti-tumor properties of the complex AuCl₂L² . The cytotoxicity against the P-388(mouse leukemia cell lines) and HL-60(human leukemia cell lines) were assessed. The activities of this compound against these two kinds of tumor cell lines were not very good. Comparing the reactivity of them, we found that their cytotoxicities have much relationship with the maintaination of the cis- structure in the substitution reaction with the ligand.