3-aryl coumarin derivative as well as preparation method and application thereof
By developing a 3-arylcoumarin derivative that highly selectively inhibits BRD4-BD2, the problems of insufficient selectivity and high toxicity of existing BRD4 inhibitors have been solved, enabling effective treatment of myocardial infarction and myocardial fibrosis.
CN121949260APending Publication Date: 2026-05-01SUN YAT SEN UNIV
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Patent Information
- Application Number
- CN202511960948.6
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2025-12-24
- Publication Date
- 2026-05-01
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Figure CN121949260A_ABST
Abstract
The invention discloses a 3-aryl coumarin derivative as well as a preparation method and application thereof, and the preparation method comprises the following steps: reacting substituted 2-bromobenzaldehyde with a substituted aryl acetic acid compound to obtain a substituted E-2, 3-diaryl acrylic acid compound; and in the presence of cuprous oxide and potassium carbonate, heating and reacting in N, N-dimethylformamide to obtain the 3-aryl coumarin derivative. The 3-aryl coumarin derivative disclosed by the invention can be combined with BRD4, has remarkable inhibitory activity on the BRD4, has a protective effect on primary myocardial cells caused by ischemia reperfusion, can inhibit proliferation, migration and invasion of cardiac fibroblasts, and can inhibit ferroptosis of hypoxia / reperfusion injury myocardial cells; the compound can be used for preparing medicines for treating diseases related to abnormal BRD4 activity.
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