Composition for prevention, amelioration, or treatment of cancer
A technology of composition and compound, which is applied in the fields of composition, prevention, and improvement of cancer, can solve the problems of adverse reactions, low specificity of cancer cells, and low cure rate of malignant tumors, and achieve the effect of inhibiting cancer metastasis
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preparation Embodiment 1-15
[0156] [Preparation Example 1-15] Synthesis of Candidate Compounds
[0157] Compounds of Preparation Examples 1-15 shown in Table 1 below were prepared using Method 1 or Method 2.
[0158] [Table 1]
[0159]
[0160]
[0161] [method 1]
[0162] The method comprises the steps of: adding an acetophenone derivative (1 equivalent), a benzaldehyde derivative (1 equivalent) and NaOH (1 equivalent) to an ethanol solvent, and then stirring at room temperature; after the reaction is completed, adding water to the reaction mixture , and then extracted with ethyl acetate; and collected the organic solvent layer, the collected material was washed once with water, washed with anhydrous MgSO 4 The washed material was dried, the solvent was distilled off under reduced pressure, and the residue was purified by silica gel chromatography.
[0163] [Method 2]
[0164] The method comprises the steps of: adding acetophenone derivatives (1 equivalent), 4-(tetrahydro-2H-pyran-2-...
Embodiment 1
[0165] [Example 1] (E)-1-(4-aminophenyl)-3-(2,4-dimethoxyphenyl)prop-2-en-1-one (YE-01)
[0166] Starting from 4-aminoacetophenone (0.30 g, 2.22 mmol), 2,4-dimethoxybenzaldehyde (0.37 g, 2.22 mmol) and NaOH (0.09 g, 2.22 mmol) according to method 1 above. The residue was purified by silica gel chromatography (developing solvent: ethyl acetate / n-hexane=1:2→1:1) to obtain the compound of Preparation Example 1 (0.15 g, yield 23.0%) as a yellow solid. R f 0.33 (ethyl acetate / n-hexane=1:1); 1 H-NMR (400MHz, CDCl 3 )δ3.85(s,3H),3.89(s,3H),6.47(d,J=2.0Hz,1H),6.52(dd,J=8.4,2.4Hz,1H),6.69(d,J=8.4 Hz, 2H), 7.55(d, J=15.6Hz, 1H), 7.56(d, J=8.8Hz, 1H), 7.92(d, J=8.4Hz, 2H), 8.02(d, J=15.6Hz, 1H); 13 C-NMR (100MHz, CDCl 3 ) 55.6, 55.7, 98.7, 105.5, 114.1, 117.8, 120.7, 129.4, 130.8, 131.1, 139.0, 150.9, 160.4, 162.8, 189.1 ppm.
Embodiment 2
[0167] [Example 2] (E)-1-(4-aminophenyl)-3-(2,5-dimethoxyphenyl)prop-2-en-1-one (YE-02)
[0168] Starting from 4-aminoacetophenone (0.50 g, 3.70 mmol), 2,5-dimethoxybenzaldehyde (0.62 g, 3.70 mmol) and NaOH (0.15 g, 3.70 mmol) according to method 1 above. The residue was purified by silica gel chromatography (developing solvent: ethyl acetate / n-hexane=1:2→1:1) to obtain the compound of Preparation Example 2 (0.66 g, yield 62.5%) as a yellow solid. R f 0.36 (ethyl acetate / n-hexane=1:1); 1 H-NMR (400MHz, CDCl 3 )δ3.81(s,3H),3.85(s,3H),4.19(br s,2H),6.69(d,J=8.8Hz,2H),6.86(d,J=8.8Hz,1H),6.91 (dd, J=8.8,2.8Hz,1H),7.16(d,J=2.8Hz,1H),7.58(d,J=15.6Hz,1H),7.92(d,J=8.8Hz,2H),8.04 (d,J=15.6Hz,1H); 13 C-NMR (100MHz, CDCl 3 ) 56.0, 56.3, 112.7, 113.9, 114.1, 116.8, 123.3, 125.2, 128.9, 131.3, 138.6, 151.2, 153.4, 153.7, 188.8ppm.
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