Synthesis And Characterization Of Takingthe Linoleic Acid As The Carrier Target To The Cancer Drugs And The Appraisalof Anticancer Treatment Activity

Cancer is the popular topic which the people study. Comparing surgery treatmentand radiotherapy to the treatment of cancer, the pharmacological treatment superioritylies in it to expand to the whole body treatment scope. Moreover, it not can only applyin the early tumor can also apply in the intermediate stage and later period tumortreatment; therefore the pharmacological treatment became the tumor treatment animportant milestone. At present, some anti-tumor medicines occupied are oftendeficient in selectivity and great in toxicity. Therefore, the design and synthesis ofselective anti-tumor medicine already becomes one of the most important topics innew anti-tumor medicine research.In this paper, the research progresses on anti-tumor medicine, linoleic acid,fluorouracil, floxuridine, paracetamol and colchicine were reviewed; five seires oftaking the linoleic acid as the carrier target to the cancer drugs’ compounds have beensynthesized; the anti-tumor activity in vivo and vitro of the compounds have beensynthesized had been preliminarily discussion. Our work mainly includes followingtwo aspects:1. Synthesis and Characteirzation on taking the linoleic acid as the carrier targetto the cancer drugsOpening linoleic acid double bond to synthesize the iodizate linoleic acid;selecting four medicines, which are fluorouracil, lfoxuridine, paracetamol andcolchicine to take the raw material, and making the coupling reaction with the linoleic acid separately. The products obtained were purified and the target compounds werech’aracterized by IR, HNMR, LC-MS and their structures accorded with the onesdesigned. Several synthetic conditions and methods were studied initially. The futrherstudy of optimized conditions and biological activity was carrying on.2. The affection of anti-tumor of the compounds have been synthesized and thetest of activity in vivo and vitroBy MTT assay, these target compounds show the activity of restraining theproliferation of SMMC-772and QGY-7703cell in vitro. Furthermore, the effect isbetter than the drugs without linoleic acid. The iodizate linoleic acid has bettercurative effect than the present iodine oil by the H22mouse liver cancer model invivo experiment.In order to further study on biological activity of anti-tumor compounds, the newtype compounds with the application prospect were filtrated. The earlier period workof our group was summarized and on the base the anti-tumor drugs was introduced tothe iodizate linoleic acid. The medicine toxicity was reduced and the efficacy ofanticancer was improved with the iodizate linoleic acid’s selectivity and targeting.