Study On Synthesis Of Porphryin Derivatives And Their Anti-tumor Activities

With good optical properties, porphyrins have been widely used as photosensitizer for clinical diagnose and photodynamic therapy of many kinds of cancer, while they have also been widely used in many other fields. Porphyrins have become the hot spot of science research. The study of photosensitizer was mainly on tetraphenyl porphyrins and its metal complex. Because exitation wavelength is short, penetrating power for animal tissue is not so good, the current photosensitizers are not fit for cancer in deep tissue.In this paper, a series of naphthylporphyrins and methylenedioxy phenylporphyrins were synthesized first for extanding exitation wavelength and reforcing penetrating power for animal tissue, The results on optical property studies of these compounds show that the introduction of naphthyl and methylenedioxy group can enhance the conjugate degree of the porphyrin to a certain extent. Further a group of ester compounds of porphyrins and small molecule acids with anti-tumor activities were synthesized.The Adler`s method was employed to synthesize naphthylporphyrins and methylenedioxy phenylporphyrins. The yields were not so high, but the prossese products were easily obtained. The ester compounds was synthesized by DCC dehydration, yields 15%～23%.Finally, MTT method in vitro was used to observe anti-tumor activities of compounds 21～28 on mouse pulmonary adenocarcinoma cells. The result show that compounds 23 and 28 have evident activity and the dosage-effect relation. The inhibition rate upto 80% at concentration 800μmol·L^-1. Compounds 5, 6, 21, 26 have no evident activity, but they are dose dependent. Compounds 24 and 27 have a little activity under the experiment concentration, but they are more active when concentration was upto a certain degree.