Study On The Synthesis And Antitumor Activity Of Carboxylic Acid Derivatives Of Ebselen

Selenium which has been called the21stamino acid is very important on life. Researchshows, selenium has extensive biological activity, and it is connected with the occurrence anddevelopment of cancer, AIDS, arthritis and other diseases, Selenium exists in a number ofallotropic forms, the most extensive research ebselen has been applied to clinical in recentyears. It has shown a variety of activities, including antitumor activity with low toxicity. Asderivatives of ebselen N-(4-carboxyphenyl)-benzisoselenazolone has the better antitumoractivity. In addition, it has been shown that1,3,4-thiadiazole derivatives possess multiplebiological activities including anticancer, antibacterial and antifungal. Moreover, theintroduction of different heterocyclic backbone to the thiadiazole nucleus will affect itsbiological activity, which has widespread attention.Based on the above ideas, a series of novel Carboxylic acid derivatives of ebselen wereprepared from N-(4-carboxyphenyl)-benzisoselenazolone and2-amino-5-substituted-1,3,4-thiadiazole by the condensation with DCC and DMAP. All synthesized compounds werestructurally characterized by IR,1H NMR, and elemental analysis. All compounds reportedherein were evaluated for in vitro antiproliferative activities against A549, SSMC-7721andPC3cell lines using CCK-8assay, contract with N-(4-carboxyphenyl)-benzisoselenazolone,the result showed that all of the eight compounds have good antiproliferative activities. Thecompound2showed better activities than other compounds against A549, the compound3,4,6showed better activities than other compounds against SSMS-7721, and the compound1,4,7gave better activities than others against PC3. This study is expected to sort new seleniumcompounds with better activity, and lay a foundation for further research on structure-activityrelationship.