Novel Dibenzo[b,d]furan-1H-1,2,4-triazole Derivatives: Synthesis and Antitumor Activity

作者：Chen, Xing; Shi, Yi-Min; Huang, Chao; Xia, Sha; Yang, Li-Juan^*; Yang, Xiao-Dong^*

来源：Anti-Cancer Agents in Medicinal Chemistry, 2016, 16(3): 377-386.

DOI：10.2174/1871520615666150817115913

• Dibenzo[b,d] furan
• 1,2,4-triazolium salts
• structure-activity relationships
• cell apoptosis

Twenty-four new dibenzo[b,d] furan-1H-1,2,4-triazole derivatives were synthesized and investigated for in vitro cytotoxic activity against five tumor cell lines. The results show that the substitution at 4-position of the 1,2,4-triazole with a benzyl, 4-bromophenacyl or naphthylacyl group could be crucial for prommoting cytotoxic activity. Especially, compound 28 was found to be the most powerful derivative with IC50 values lower than 3.50 mu M against five investigated tumor cell lines, while compound 19 showed selective activity against leukemia (HL-60) and breast carcinoma (MCF-7) cell lines with IC50 values of 0.80 and 1.76 mu M, respectively. Compound 19 can induce cell cycle arrest at G2/M phase and apoptosis in SMMC-7721 cells.

• 出版日期2016
• 单位云南民族大学; 云南大学