Chalcone tryptophan derivatives capable of improving renal toxicity of cis-platinum and anti-tumor activity
A technology of chalcone derivatives and drugs, which is applied in the direction of antineoplastic drugs, organic active ingredients, inorganic active ingredients, etc., can solve the problems of low efficacy, low selectivity, and limited side effects of chalcone compounds, and achieve kidney cell Damage improvement, toxicity reduction, good inhibitory effects
- Summary
- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
Method used
Image
Examples
Embodiment 1
[0036] The preparation of embodiment 1 compound 1
[0037]
[0038] Concrete preparation steps are as follows:
[0039] A solution of p-methoxybenzaldehyde (3.3mmol) and 4-acetobenzoic acid (3.0mmol) in acetic acid (20ml) was added with 5-6 drops of concentrated sulfuric acid and stirred at 60°C for 48h. The reaction mixture was then poured into 200 ml of cold water. The precipitated product was filtered and recrystallized from methanol to obtain intermediate 2a. Then 2a (3 mmol), methyl tryptophan hydrochloride (3.3 mmol) and triethylamine (7.9 mmol) were added into 50 mL of dry dichloromethane and stirred at 0° C. for 30 min. Then add 3-(3-dimethylaminopropyl)-1-ethylcarbodiimide hydrochloride (EDCI) (3.3mmol) and 1-hydroxybenzotriazole (HOBt) (0.33mmol), under nitrogen After stirring at room temperature for 24 h, the reaction mixture was washed with 5% HCl. The organic phase was concentrated under vacuum to give intermediate 3a. Then, 3a was mixed with methanol / wate...
Embodiment 2
[0045] The preparation of embodiment 2 compound 2
[0046]
[0047] Concrete preparation steps are as follows:
[0048] A solution of p-methoxybenzaldehyde (3.3mmol) and 4-acetobenzoic acid (3.0mmol) in acetic acid (20ml) was added with 5-6 drops of concentrated sulfuric acid and stirred at 60°C for 48h. The reaction mixture was then poured into 200 ml of cold water. The precipitated product was filtered and recrystallized from methanol to obtain intermediate 2a. Then 2a (3 mmol), methyl tryptophan hydrochloride (3.3 mmol) and triethylamine (7.9 mmol) were added into 50 mL of dry dichloromethane and stirred at 0° C. for 30 min. Then add 3-(3-dimethylaminopropyl)-1-ethylcarbodiimide hydrochloride (EDCI) (3.3mmol) and 1-hydroxybenzotriazole (HOBt) (0.33mmol), under nitrogen After stirring at room temperature for 24 h, the reaction mixture was washed with 5% HCl. The organic phase was concentrated under vacuum to give intermediate 3a. Then 3a was mixed with methanol / water...
Embodiment 3
[0054] The preparation of embodiment 3 compound 3
[0055]
[0056] Concrete preparation steps are as follows:
[0057] A solution of p-methoxybenzaldehyde (3.3mmol) and 4-acetobenzoic acid (3.0mmol) in acetic acid (20ml) was added with 5-6 drops of concentrated sulfuric acid and stirred at 60°C for 48h. The reaction mixture was then poured into 200 ml of cold water. The precipitated product was filtered and recrystallized from methanol to obtain intermediate 2a. Then 2a (3 mmol), methyl tryptophan hydrochloride (3.3 mmol) and triethylamine (7.9 mmol) were added into 50 mL of dry dichloromethane and stirred at 0° C. for 30 min. Then add 3-(3-dimethylaminopropyl)-1-ethylcarbodiimide hydrochloride (EDCI) (3.3mmol) and 1-hydroxybenzotriazole (HOBt) (0.33mmol), under nitrogen After stirring at room temperature for 24 h, the reaction mixture was washed with 5% HCl. The organic phase was concentrated under vacuum to give intermediate 3a. Then, 3a was mixed with methanol / wate...
PUM
Login to View More Abstract
Description
Claims
Application Information
Login to View More