Synthesis And In Vitro Antitumor Activity Of1,3,4-thiadiazole Derivatives Based On Selenazole

Selenium is one of the indispensable trace elements in human body. It exists in differentenzyme systems as components and participates in various mechanism like anti-oxidation,anti-radiation and anti-tumor. Besides, the pathological process of certain diseases such ascardiovascular disease and cancer can be inhibited effectively by selenium.Selenazole is reported to possess diverse biological activities in processes related toinflammation control, brain dysfunction cure and cardiovascular protection, which isattributed to the heterocyclic structure composed by selenium and nitrogen in the moleculeand thus gains better affinity to certain receptors. Drugs like ebselen and selenazofurin arerepresentatives with decent anti-cancer activity that function in this manner. In fields likeinsecticide, sterilization, anti-inflammation and anti-tumor,1,3,4-thiadiazole is widely appliedbecause of its potential active center, which is formed by the basic structure of ‘C-N-S’connection mode in the molecule. This special structure can chelate some important metallicions in human body, facilitate transportation and absorption process and thus improvebio-activity. Amide derivatives has the ability to inhibit the growth of bacteria, fungus andcancer cells, especially when a bisamide structure is formed by connecting aromatic orheterocyclic structure together. It’s reported that heterocycles bridged by electron-donatingatoms(i.e.O,S) shows stronger affinity between receptors and ligands, which can be guidancein structure modification of selenazole, thiadiazole and amide derivatives.According to the theory of fragment-based drug design, we synthesized series of1,3,4-thiadiazole derivatives based on selenazole and tested their in vitro anti-tumor activityagainst L1210cell(leukemic) and MCF-7cell(human breast cancer cells) using CCK-8method. Results indicated that tested samples reacted to different cancer cells with selectivity,while most samples showed strong anti-cancer activity against MCF-7cell and even strongerthan reference sample2-phenyl-4-selenazole carboxylic acid, the anti-cancer activity againstL1210cell was relatively weak. This conclusion lays foundation for further design andscreening of anti-cancer drugs.