Synthesis and antitumor effects of a new class of 1,2,4-triazole derivatives

In order to obtain more effective antitumor agents, a new class of 1,2,4-triazole derivatives bearing disulfide bond were designed and synthesized. All the final compounds were confirmed by IR, 1 H NMR, 13 C NMR and HR-ESI-MS. The in vitro cytotoxicity of the compounds on the SMMC-7721, Hela, A549 cancer cell lines and the L929 normal cell lines were assessed by cell counting kit-8 (CCK-8). Many of tested compounds 8a–h , 9a–h , 10a–h had better cytotoxic activity on various cancer cell lines than positive control 5-fluorouracil, and they were less cytotoxic to normal cell line L929 than cancer cells. Among them, compounds 9e , 9g , and 10h showed better cytotoxic activity on SMMC-7721 cells with IC 50 values 4.12, 2.92, and 4.53 μM, respectively. Compounds 8a , 9g , 10g and 10h displayed high antiproliferative activity against Hela cells with IC 50 values 6.31, 4.31, 6.31 and 3.97 μM, respectively. Compounds 8c , 10a and 10h revealed effective biological potency on A549 cells with IC 50 values 4.75, 4.92 and 3.73 μM, respectively. Moreover, a great majority of tested compounds revealed low cytotoxicity on normal cell line L929.