Design, synthesis and biological evaluation of novel 3-alkylsulfanyl-4-amino-1,2,4-triazole derivatives
Design, synthesis and biological evaluation of novel 3-alkylsulfanyl-4-amino-1,2,4-triazole derivatives
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新型3-烷基硫基-4-氨基-1,2,4-三唑衍生物的设计、合成及生物学评价
DOI：
10.1016/j.bmcl.2016.05.086
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发表时间：
2016
影响因子：
2.7
通讯作者：
You Wen-Wei
中科院分区：
文献类型：
--
作者：
Zhao Pei-Liang;Chen Peng;Li Qiu;Hu Meng-Jin;Diao Peng-Cheng;Pan En-Shan;You Wen-Wei
Based on our previous work, a series of novel 3-alkylsulfanyl-4-amino-1,2,4-triazole derivatives were designed, synthesized and evaluated for their antiproliferative activities. The results indicated that some compounds possessed significant antiproliferative activities against four cancer cell lines, HepG2, HCT116, PC-3, and Hela. Particularly, the most promising compound8ddisplayed 184-, 18-, and 17-fold improvement compared to fluorouracil in inhibiting HCT116, Hela and PC-3 cell proliferation with IC50values of 0.37, 2.94, and 31.31 μM, respectively. Most interestingly, the compound did not affect the normal human embryonic kidney cells, HEK-293. Moreover, mechanistic investigation showed that the representative compound8dinduced apoptosis and blocked cell cycle in G2/M phase in Hela cells in a dose-dependent manner. These findings suggest that compound8dmay have potential to be developed as a promising lead for the design of novel anticancer small-molecule drugs.
