一种咪唑并[3,4-d]嘧啶类化合物及其合成方法与应用
By synthesizing imidazo[3,4-d]pyrimidine compounds to target and inhibit palmitoyltransferase of DHHC protein, the problem of insufficient selectivity and activity of existing DHHC inhibitors has been solved, achieving effective inhibition of tumor cells and making it suitable for development as an anti-tumor drug.
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- HEBEI UNIVERSITY
- Filing Date
- 2024-01-19
- Publication Date
- 2026-07-17
AI Technical Summary
Existing DHHC inhibitors are mostly non-selective and have weak activity, making it difficult to effectively inhibit the growth of tumor cells. Furthermore, current research on palmitoylation modification in regulating PD-L1 stability has not yet yielded significant breakthroughs.
An imidazo[3,4-d]pyrimidine compound was designed and synthesized. Through computer-aided drug design and molecular simulation, it was used to target and inhibit palmitoyltransferase of DHHC protein, thereby inhibiting the palmitoylation process of substrate protein. This compound was used as a palmitoyltransferase inhibitor to inhibit the proliferation of tumor cells.
This compound exhibits varying degrees of anti-proliferative activity against a variety of cancer cells, with some compounds showing even better inhibitory activity against cancer cells than the positive control drug cisplatin, demonstrating its potential to be developed into a new generation of anti-tumor drugs.
Smart Images
Figure CN118063472B_ABST