Wang, Xiao-Meng published the artcileSynthesis and antitumor activities evaluation of m-(4-morpholinoquinazolin-2-yl)benzamides in vitro and in vivo, Application of N-Methyl-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzamide, the publication is European Journal of Medicinal Chemistry (2015), 382-395, database is CAplus and MEDLINE.
In the present study, a series of m-(4-morpholinoquinazolin-2-yl)benzamides were designed, synthesized, and characterized. The antiproliferative activities of the synthesized compounds were evaluated against two human cell lines (HCT-116 and MCF-7). Compounds with IC50 values below 4 μM were further evaluated against U-87 MG and A549 cell lines. Among these evaluated compounds, compound I displayed a remarkable antiproliferative effect in vitro. The hoechst staining assay showed that compound I caused morphol. changes. The cell cycle and apoptosis assay further indicated that compound I can arrest HCT-116 cells in G2/M and G0/G1 phase and induce apoptosis. PI3K enzyme assays indicated that compounds I and II selectively inhibit PI3Kα. A Western bolt assay further suggested that compound I can block the PI3K/Akt/mTOR pathway. Moreover, compound I inhibited tumor growth on a mice S180 homograft model. These findings directly identify m-(4-morpholinoquinazolin-2-yl)benzamide derivatives as novel anticancer agents.
European Journal of Medicinal Chemistry published new progress about 1197171-76-8. 1197171-76-8 belongs to amides-buliding-blocks, auxiliary class Boronic acid and ester,Amine,Benzene,Amide,Boronate Esters,Boronic Acids,Boronic acid and ester,, name is N-Methyl-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzamide, and the molecular formula is C18H28B2O4, Application of N-Methyl-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzamide.
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