Design, synthesis and biological evaluation of novel 3-alkylsulfanyl-4-amino-1, 2, 4-triazole derivatives. Issue 15 (1st August 2016)

• Record Type: Journal Article
• Authors: Zhao, Pei-Liang; Chen, Peng; Li, Qiu; Hu, Meng-Jin; Diao, Peng-Cheng; Pan, En-Shan; You, Wen-Wei
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 15(2016)
• Page Start: 3679
• Page End: 3683
• Publication Date: 2016-08-01
• Subjects: 1, 2, 4-Triazole -- Alkylsulfanyl -- Synthesis -- Antiproliferative activity; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.05.086
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: 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 compound8d displayed 184-, 18-, and 17-fold improvement compared to fluorouracil in inhibiting HCT116, Hela and PC-3 cell proliferation with IC50 values 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 compound8d induced apoptosis and blocked cell cycle in G2 /M phase in Hela cells in a dose-dependent manner. These findings suggest that compound8d may have potential to be developed as a promising lead for the design of novel anticancer small-molecule drugs.