N-benzyl-alpha-amino amides as late phase anaphase promoting complex / cyclosome (apc / c) inhibitors
By combining compound I with proTAME for administration, the resistance problem caused by abnormal overdose of Cdc20 protein in breast cancer treatment in existing technologies has been solved, achieving highly efficient inhibition and toxicity against cancer cells, especially effective treatment of breast cancer cells.
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- 科学研究高级委员会(CSIC)
- Filing Date
- 2021-12-16
- Publication Date
- 2026-06-19
AI Technical Summary
Existing cancer treatments, especially for breast cancer, are ineffective at inhibiting the abnormal overproduction of Cdc20 protein and the abnormal signal transduction at the spindle assembly checkpoint, leading to resistance to traditional microtubule-disrupting drugs. Therefore, there is a need to develop new APC/C inhibitors.
The development of Formula I compounds and pharmaceutical compositions thereof, which inhibit the function of APC/C by binding to the Cdc20 protein, including enhanced inhibitory effects on cancer cells when administered in combination with proTAME.
It enhanced the cytotoxic effect on cancer cells, especially the inhibitory effect on breast cancer cells, and showed higher cytotoxicity and colony formation inhibition ability, demonstrating the potential therapeutic value of compound o-TFB-Tyr for different types of cancer.
Smart Images
Figure CN116583497B_ABST