Metalloporphyrins - 5 - Fluorouracil Compounds Synthesis And Biological Activity

In order to improve the target activity of anticancer medicine and reduce their untoward effccts,the effective drug is expected with high selectivity,which means it can distinguish target cell from normal cell properly. Porphyrin and melalloporphyrins have special affinity with cancer cell because 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.So the research on the use of porphyrin and metalloporphyrins for tumor localization and therapy have caused great interests of chemists,medicals and biologists.5-Fluorouracil is a kind of popular antimetabolic drug used in clinic.It has the similar structure with uracil which is necessary to the cancer cell.It contents with uracil in the same enzyme system,blocks the metabolic link,impeds the synthesis of DNA,and then prohibits the propagation of the cancer cells.As a kind of antitumor drug,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 synthesized a series of porphyrin-5-Fluorouracil and metalloporphyrin-5-Fluorouracil compounds.We expected these compounds can reach tumor tissue and collect and kill cancer cell directly,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 twelve porphyrin-5-Fluorouracil compounds and four novel manganese-5-Fluorouracil compounds.At the same time, we initially explored the four manganese-5-Fluorouracil compounds' in vitro antitumor activities.The results are as follows:In the first part,twelve porphyrin-5-Fluorouracil compounds have been prepared.That is,Phenylporphyrin substituted by chloride at different position and 5-Fluorouracil were linked up by different hydrocarbon chain(C2,C3,C4).The structures of twelve porphyrin-5-Fluorouracil compounds have been characterized by UV,IR,1HNMR and MS.Porphyrin-5-Fluorouracil compounds occurred complexation reaction with manganese and four novel manganese-5-Fluorouracil compounds have been obtained.Their structures have been determined by UV and 1R.In the second part,the in vitro antitumor activities of manganese-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.