Synthesis Of Chlorin 5 - Fluorouracil Derivatives

Porphyrins have special affinity with cancer cell because of its distinctive structure. They can be taken up and retained by tumor tissues selectively. So the research on the use of porphyrin for tumor localization and therapy have caused great interests of chemists,medicals and biologists.5-Fluorouracil is a kind of popular anti-metabolic drug used in clinic.It has the similar structure with uracil which is necessary to the cancer cell.It completes with uracil in the same enzyme system, blocks the metabolic link, impedes the synthesis of DNA, and then prohibits the propagation of the cancer cell.As a kind of anti-tumor 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 improve the target activity of anticancer medicine and reduce their untoward effects,people often connect photosensitizers--Porphyrin which can be taken up and retained by tumor tissue selectively with 5-Fluorouracil,.We expected these compounds can reach tumor tissue and collect and kill cancer cell directly ,so as to improve the curative effect.Compared with Porphyrin,chlorines,as a second generation photosensitizers, has better character:an enhanced absorption in far red region, shorter remain time,smaller untoward effects and so on. With the appropriate light, the use of chlorins for therapy will have better achievement.In this paper,we synthesized and charactered seven new chlorins compounds and four novel chlorins -5-Fluorouracil compounds. The results are as follows:In the first part, we synthesized seven novel chlorines, four chlorin-5-Fluorouracil compounds. The structures of these compounds have been characterized by UV, IR, ~1HNMR and MS.In the second part,optimum reaction and separation conditions have been researched and improved .There are still further work to be done, such as invitro anti-tumor activities test of the eleven compounds.In the third part ,we studied the fluorescent properties on the novel chlorines. The results indicate that the fluorescence spectra of the chlorines is stronger than porphyrins'.