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

Bioorganic & Medicinal Chemistry Letters
Xiao-Meng WangSan-Qi Zhang

Abstract

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 10μM 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.

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Citations

Nov 28, 2015·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Mingyan YangMingan Wang
Mar 23, 2017·Bioorganic & Medicinal Chemistry Letters·Minhang XinSan-Qi Zhang
Oct 13, 2018·Chembiochem : a European Journal of Chemical Biology·Akop YepremyanEric E Simanek
Jul 13, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Emily W WrightMark E Welker
Jul 6, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Ronald A NelsonMark E Welker
Oct 4, 2019·European Journal of Medicinal Chemistry·Fatma M ElmenierKhaled A M Abouzid
Apr 23, 2020·Bioorganic & Medicinal Chemistry Letters·Hao-Yue XiangChun-Hao Yang

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