2-苯基-4-胺基喹唑啉类化合物或其可药用盐及其制备方法和应用
By designing 2-phenyl-4-aminoquinazoline compounds to enhance binding affinity and water solubility to CYP1B1 enzyme, the problem of insufficient selectivity of existing inhibitors was solved, achieving efficient and selective inhibition of CYP1B1.
CN117924190BActive Publication Date: 2026-07-17CHONGQING MEDICAL UNIVERSITY
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- CHONGQING MEDICAL UNIVERSITY
- Filing Date
- 2024-01-19
- Publication Date
- 2026-07-17
AI Technical Summary
Technical Problem
Existing CYP1B1 inhibitors have low selectivity for CYP1B1, and inhibiting CYP1B1 also inhibits CYP1A1 and CYP1A2, limiting their further development.
Method used
We designed and synthesized 2-phenyl-4-aminoquinazoline compounds, which enhanced the binding affinity to CYP1B1 enzymes by strengthening the π-π stacking effect and the electronic conjugation of the amino group, and can generate water-soluble hydrochloride to improve water solubility.
Benefits of technology
It achieved highly efficient inhibition of CYP1B1, with an IC50 value of 4.14×10-5 nM, which is much higher than existing inhibitors. At the same time, it has high selectivity for CYP1B1, and the IC50 values for CYP1A1 and CYP1A2 are 2.07×106 and 3.62×107 times, respectively.
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Figure CN117924190B_ABST
Abstract
本发明属于疾病治疗药物技术领域，具体涉及一种2‑苯基‑4‑胺基喹唑啉类化合物或其可药用盐及其制备方法和应用。2‑苯基‑4‑胺基喹唑啉类化合物的结构式为：其中，R1、R2、R3和R4分别独立选自氢、卤素、烷基或卤代烷基；R5和R6均为H或者R5和R6形成苯环。该化合物或其盐对CYP1B1具有较高的抑制效率；同时还有较高选择性。
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