Synthesis Of Phenylporphyrin-5-Fluorouracil Derivatives And The Study Of Anticancer Activities

The malignant tumour is common and frequently-occurring disease that seriously harms mankind's health. According to the lasterest investigation of China Health Ministry , in the city, the head of the ten cause of death of resident is the malignant tumour, and in the rural area, it also is preceding 3 of the ten cause of death of resident. At present this kind of disease has become a great research subject in the world medical science domain.5-Fluorouracil is a kind of popular antimetabolic drug used in clinic. 5-Fluorouracil has inhibition effect on many kinds of cancer, but it also seriously hurts the normal cells while it kills the cancer cells. In order to decrease the toxicity of 5-Fluorouracil, we need synthesize a series of porphyrin-5-Fluorouracil and metalloporphyrin-5-Fluorouracil compounds. Porph- yrin and metalloporphyrins have special affinity with cancer cell because of their distinctive structure. They can be taken up and retained by tumor tissue selectively. With the appropriate light, they can produce fluorescence and kill the cancer cell.In order to decrease the toxicity of 5-Fluorouracil , we connect porphyrin to 5-Fluorouracil with longer carbochain , synthesizing eight porphyrin-5-Fluorouracil and eight metalloporphyrin-5-Fluorouracil compounds.We expected these compounds can reach tumor tissue directly and kill cancer cell,so as to improve the curative effect.Furthermore, they cure cancer coordinating laser technology at the position of the body which the laser can reach for better curative effect.In this paper,we synthesized and charactered eight porphyrin-5-Fluorouracil compounds and eight novel zinc-5-Fluorouracil compounds. The results are as follows:1,In the first part,We synthesis eight phenylporphyrin substituted by chloride and then link 5-Fluorouracil by hydrocarbon chain in different length(C5,C6).The structures of eight porphyrin-5-Fluorouracil compounds have been characterized by UV, IR, 1HNMR and MS. Porphyrin-5-Fluorouracil compounds occurred complexation reaction with Mn and eight novel Mn-5-Fluorouracil compounds have been obtained.Their structures have been determined by UV and IR.2,In the second part ,optimum reaction and separaion conditions have been reaserched and improved.3,Optimum reaction and separaion conditions have been reaserched and improved. And the in vitro antitumor activities of Mn-5-Fluorouracil compounds have been tested by MTT.The experimental results indicates that these compounds show good performance in anticancer activities.The further work still need to be done.