Polθ抑制剂及其制备方法、药物组合物和应用
By designing and synthesizing a novel Polθ inhibitor, the problem of the lack of effective Polθ inhibitors in the existing technology has been solved, and effective inhibition of Polθ enzyme has been achieved. This inhibitor can be used to treat cancers such as breast cancer and ovarian cancer, and has a widely applicable and easily scalable preparation method.
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- CHINA PHARM UNIV
- Filing Date
- 2023-07-13
- Publication Date
- 2026-07-17
AI Technical Summary
There are currently no effective Polθ inhibitors for the treatment of various human cancers, such as breast cancer, ovarian cancer, lung cancer, and colorectal cancer. Polθ is overexpressed in these cancers but underexpressed in healthy tissues, making it a potential anti-tumor target.
A class of novel Polθ inhibitors were designed and synthesized, and prepared into pharmaceutical compositions through specific chemical reactions to inhibit Polθ enzyme activity. This process includes a multi-step compound synthesis process and a pharmaceutically acceptable salt form, which can be applied to anti-tumor drugs.
This Polθ inhibitor can effectively inhibit Polθ enzyme activity, with an IC50 value reaching the nanomolar level. It is widely used in the preparation of drugs for treating cancers such as breast cancer and ovarian cancer, and the preparation method is highly applicable and easy to expand the structure.
Smart Images
Figure CN117510462B_ABST