Synthesis And Anticancer Activitives Of 2-[(2'-chloro-6'-fluorophenyl)amino]-5-methylphenyl Acetas

Cyclooxygenase2(COX-2) is involved in the progression of colorectal tumor. The evidence provide convincing evidence that NSAIDs can inhibit colorectal cancer cell formation and growth. Clinical evidence indicates that COX-2-specific inhibitors show equivalent or greater efficacy in colorectal cancer prevention compared with NSAIDs.Lumiracoxib is a novel COX-2 inhibitor chemically distinct from the other COX-2-sp- ecific inhibitors by virtue of the presence of a carboxylic acid group, making it a weakly acidic molecule. Although Lumiracoxib have been shown to be less toxic to the gastrointestinal tract than NSAIDs, its cardiovascular safety profile is questioned. In the study of the synthesis of Lumiracoxib, we observed that it can inhibit the growth of K562 cell line, which indicate it have anti-tumor activity.Thirteen esters derivatives of Lumiracoxib have been designed base on the principle of prodrug. The aim of esterification is to elevate the bioavailability and safety of. Lumiracoxib. We desire that these derivatives might inhibit colorectal cancer cell formation and growth. Preparing Lumiracoxib, the yield of step 2 and step 4 were improved. The target esters were synthesized by DCC. Their chemical structures of the target compounds were confirmed by elemental analysis, IR and 1H-NMR. The antitumor activities of the target compound were tested in vitro by the MTT assay. The preliminary pharmacological tests showed these compound cannot inhibit colorectal cancer cell growthing efficiently.