Studies On Synthesis And Biological Activities Of Porphyrins Containing Mercaptopurine Substituents

Porphyrins have enrichment around the cancer tissues and special binding activity toward malignant cells, while the Mercaptopurine of nucleotide family is a kind of drugs clinically used to cure the leukemia. It was possible to get porphyrin compounds with higher anticancer activity and specification toward malignant tissues if they were combined into one molecule. But the key to get such kind of compound is synthesis. The synthesis method of the porphyrins containing Mercaptopurine molecules would greatly influence the study and application of the compounds. So this thesis are centered on method of synthesize such kind of porphyrins and their bioactivities. According to the theories and methods of drugs (designing analog design and combination principles), the aim of this thesis is to design and synthesize new compounds containing anticancer groups, including 7 kinds of porphyrins bearing Mercaptopurine molecules and to preliminarily investigate their bioactivities and anticancer activities toward leukemia cells, liver cancer cells and mammary cancer cells. Details as follows:1. According to the theories and methods of drugs (designing analog design and combination principles), Total synthesized 7 kinds of new porphyrins containing Mercaptopurine molecules. 7 kinds of new intermediates were also synthesized during the total synthesis. Use 1, 2-dibroethane as a bridge we linked porphyrins and Mercaptopurine molecules together easily, and find a new way to synthesize new kinds of guided-drugs simple and convenient.2. Investigation of the biological activities. In order to examine the anticancer activities of porphyrins containing different amount of Mercaptopurine molecules, three kinds of tumor cells including leukemia, liver cancer and mammary cancer cells were cultivated to measure the activities of the new porphyrins using MTT method. The relationship between structure and activities was studied by investigation of anticancer activities of substituted porphyrins toward malignant tissues.