A piperazine-1-methylindole-2-carboxamide derivative, its preparation method and application

By synthesizing piperazine-1-methylindole-2-carboxamide derivatives and their salts, the problems of low response rate and drug resistance of existing anticancer drugs have been solved, and effective inhibition of various cancer cells and STAT3 protein phosphorylation have been achieved, with significant anti-cancer effects.

CN118772123BActive Publication Date: 2025-09-16HENAN RADIOMEDICAL SCI & TECH CO LTD
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Patent Information

Application Number
CN202410765958.3
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2024-06-14
Publication Date
2025-09-16
Estimated Expiration
2044-06-14

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Abstract

The present invention discloses a piperazine-1-methylindole-2-formamide derivative, a preparation method and an application thereof, and belongs to the field of drug synthesis. The piperazine-1-methylindole-2-formamide derivative structural formula is shown in general formula I: wherein R1 is selected from n=1,2,3,4,5,6,7,8,9,10. The biologically active piperazine-1-methylindole-2-formamide nucleus group contained therein is further chemically modified to produce many biologically more active compounds, which expands the wide application of such compounds in biomedicine and the development prospects of pharmaceutical preparations. Such compounds can significantly inhibit the proliferation of cells such as breast cancer, liver cancer, pancreatic cancer, gastric cancer, lung cancer, esophageal cancer, cervical cancer, multiple myeloma, diffuse large B-cell lymphoma at low doses (nanomolar), and can effectively inhibit STAT3 protein phosphorylation, indicating that such compounds have the prospect of being developed as anti-tumor drugs.
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