Design, synthesis and antiproliferative activity evaluation of m-(4-morpholinyl-1,3,5-triazin-2-yl)benzamides in vitro

作者：Wang, Xiao-Meng; Xu, Jing; Xin, Min-Hang; Lu, She-Min; Zhang, San-Qi^*

来源：Bioorganic & Medicinal Chemistry Letters, 2015, 25(8): 1730-1735.

DOI：10.1016/j.bmcl.2015.02.067

• Benzamide
• 1,3,5-Triazine
• Synthesis
• Antiproliferative activity

In the present study, a series of m-(4-morpholino-1,3,5-triazin-2-yl)benzamides were designed, synthesized and characterized. Their antiproliferative activities against HCT-116 cell and MCF-7 cell at 10 mu M were evaluated by MTT assay. Compounds T6, T10, T11, T12 and T19 exhibited potent antiproliferative activities. Thus, their IC50 values against HCT-116 cell, MCF-7 cell, Hela cell, U-87 MG cell and A549 cell were measured. The SAR of the target compounds was preliminary discussed. The Western bolt assay suggested that compound T11 can block the PI3K/Akt/mTOR pathway. Hoechst staining assay indicated that compound T11 can cause morphological changes and induce apoptosis of HCT-116 cells. These findings directly identify the m-(4-morpholinyl-1,3,5-triazin-2-yl)benzamide derivatives as novel antiproliferative agents and further verify the value of the benzamide fragment in drug design.

• 出版日期2015-4-15
• 单位西安交通大学