Chemical compound for preparation of anti-breast-cancer drugs as well as preparation method and application of chemical compound
An anti-breast cancer, compound technology, applied in the field of compounds containing cinnamic acid skeleton, can solve the problem of incomplete understanding of the etiology of malignant tumors
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Embodiment 1
[0020] Dissolve 3.36g (15mmol) of compound A in 50mL of dichloromethane in a 100mL round-bottomed flask, then add 100mmol of triethylamine, then add 25mmol of methanesulfonyl chloride dropwise at 0°C under nitrogen protection, and stir while adding dropwise. After 20 minutes, it was allowed to rise to room temperature naturally, and the stirring was continued for 0.5 hour. Then add 100mL dichloromethane, wash with distilled water 100mL × 3 times, dry over anhydrous sodium sulfate, concentrate the organic phase under reduced pressure, and finally use silica gel column chromatography to purify, eluent is petroleum ether / ethyl acetate=2: 1, to obtain oily compound B, ESI-MS, m / e=380.02 ([M+NH 4 ] + ).
[0021] Dissolve 15 mmol of compound C in 50 mL of DMF, add 13 mmol of oily compound B obtained in the previous step, stir at 80°C for 2 hours, add 200 mL of distilled water to quench, and the reaction is complete. The reaction solution was washed with saturated brine 100mL×3 ti...
Embodiment 2
[0030] The maximum tolerance test of the formula I compound of the present invention:
[0031] Get 40 mice with a body weight of 20 ± 2g, half male and half male, orally administered at 0.8mg / 20g such as a suspension with a concentration of 100mg / ml of the compound of formula I, and continuously observe the death of the animal within 30 days. As a result, within 30 days , all animals had normal feeding activity, no deaths, no LD detected 50 , considered non-toxic.
Embodiment 3
[0033] The test of the antitumor cell activity of the compound described in formula I of the present invention
[0034] The growth inhibitory effect of compound I on human breast cancer cell lines was evaluated by MTT assay.
[0035] 1. Main reagents and methods:
[0036] Cells in the logarithmic phase of growth: human breast cancer cell lines MCF-7, 4T1, MDA-MB-231, MCF-7B (purchased from the Cell Bank of the Chinese Academy of Sciences at 1.5 × 10 4 Concentrations were seeded in 96-well plates. ) Absorb the original culture medium after the cells adhere to the wall for 24 hours. The experiment was divided into blank control group and drug treatment group. The blank group was replaced with 1640 medium containing 10% fetal bovine serum; the drug-treated group was replaced with the medium containing compound I at concentrations of 100 μm, 50 μm, 10 μm, 1 μm, 0.1 μm, 0.01 μm, and 0.001 μm. After culturing for 48 hours, add MTT at a concentration of 5 mg / mL, and continue to s...
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