27656-94-6Relevant academic research and scientific papers
Synthesis and biological evaluation of disulfides bearing 1,2,4-triazole moiety as antiproliferative agents
Wang, Xue-Feng,Zhang, Shuai,Li, Bao-Lin,Zhao, Ji-Jun,Liu, Yu-Ming,Zhang, Rui-Lian,Li, Bo,Chen, Bao-Quan
, p. 3367 - 3374 (2017)
A series of novel nonsymmetrical disulfides bearing 1,2,4-triazole moiety were designed, synthesized, and evaluated for their in vitro antiproliferative activities against human cancer cell lines SMMC-7721, Hela, A549, and normal cell lines L929 by CCK-8 assay. The preliminary bioassay results demonstrated that most of the tested compounds 8a–r exhibited good antiproliferative activities, and some compounds showed better effects than positive control 5-fluorouracil against various cancer cell lines. Among these compounds, compound 8l showed significant antiproliferative activity against SMMC-7721 cells with IC50 value of 2.97 μM. Compound 8f displayed highly effective biological activity against Hela cells with IC50 value of 3.51 μM. Compound 8d exhibited the best inhibitory effect against A549 cells with IC50 value of 2.79 μM. Furthermore, some of the tested compounds showed weak cytotoxic effect against the normal cell lines L929. The pharmacological results suggest that the substituent groups are vital for improving the potency and selectivity of this class of compounds.
Synthesis and antitumor effects of a new class of 1,2,4-triazole derivatives
Wu, Zheng,Li, Xin,Chi, Chun-Lan,Xu, Lu,Sun, Yong-Yue,Chen, Bao-Quan
, p. 142 - 151 (2020/10/22)
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, 1H NMR, 13C 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 IC50 values 4.12, 2.92, and 4.53 μM, respectively. Compounds 8a, 9g, 10g and 10h displayed high antiproliferative activity against Hela cells with IC50 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 IC50 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.
