Synthesis And Properties Of 1, 2, 3-Triazole Linked Porphyrin Cytidines

Cancer is one of the diseases which affect human beings'health. There are many ways to cure cancer, among them anticancer drug is one of the most effective ways. But anticancer drugs used by now mostly have the disadvantage that they can not be directionally transported to the cancer cells. They not only kill the cancer cells but also damnify partly the normal cells severely. Therefore, it is an important issue in medicine and pharmacology to develop new anticancer drugs which are more active and specific in killing the cancer cell. In this thesis, according to the prodrug principle and that porphyrin can accumulate in neoplasm cell rather than surrounding normal cell, 1, 2, 3-triaole linked porphyrin-cytidines were designed and synthesized via Sharpless-Huisgen 1, 3-cycloaddtion and their biological activities were studied prelimilarily.The main contents were summarized as following:(1) According to the literature, the mechanism of porphyrins'direction in cancer cells and the application progress of porphyrin and cytidine in anticancer researches were reviewed. Also the principle of Click Chemistry and the application of 1, 2, 3-triazoles in medicinal fields were summaried in detail.(2) 1, 2, 3-triaole linked porphyrin-cytidines were designed and synthesized via Sharpless-Huisgen 1, 3-cycloaddtion based on the principle of prodrug and were charactered by NMR, UV, IR, and MS.(3) MTT method was selected to study their anticancer properties in vitro of above synthesized 1, 2, 3-triaole linked porphyrin-cytidines. The result showed that these compounds can inhibit the MCF-7 cancer cell in low dose.(4) The interactions between above synthesized porphyrin-cytidines and BSA by fluorescence spectra were studied and the experimental results show that porphyrins can enter into the hydrophobic cavity of BSA by the hydrophobic force to form a stable complex.