Novel 4-(1H-pyrrole-3-yl) pyrimidine anti-breast cancer compound and preparation method thereof
By designing and synthesizing 4-(1H-pyrrolo-3-yl)pyrimidine compounds, the problems of poor selectivity and insufficient pharmacokinetic properties of existing USP7 inhibitors were solved, achieving efficient inhibition of USP7 and improved pharmacokinetic properties.
CN122255109APending Publication Date: 2026-06-23HAINAN MEDICAL UNIV
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Patent Information
- Application Number
- CN202610520633.8
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2026-04-20
- Publication Date
- 2026-06-23
AI Technical Summary
Technical Problem
Existing USP7 inhibitors suffer from poor selectivity and insufficient pharmacokinetic properties, making them difficult to use effectively in the development of anti-tumor drugs.
Method used
A series of 4-(1H-pyrrolo-3-yl)pyrimidine compounds were designed and synthesized, and their selectivity and pharmacokinetic properties for USP7 were improved through specific structural modifications, including the flexibility of using the pyrimidine ring as the pharmacophore and the pyrrolo ring as the modification site.
Benefits of technology
It achieves highly efficient inhibitory activity against USP7, while improving selectivity for family enzymes and the pharmacokinetic properties of the compound, such as metabolic stability and blood-brain barrier penetration.
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Abstract
The invention belongs to the technical field of medicines, and relates to a novel 4-(1H-pyrrole-3-yl) pyrimidine anti-breast cancer compound and a preparation method thereof. The heterocyclic ring system is different from a common known inhibitor parent nucleus, the pyrimidine ring of the heterocyclic ring system can be used as a key pharmacophore to interact with a catalytic domain, and the introduction of the pyrrole ring provides a flexible modification site for exploring the physicochemical properties of allosteric regulation or fine regulation molecules. The invention aims at performing efficient structure-function relationship optimization on the skeleton, and aims at remarkably improving the selectivity of the skeleton to enzymes in the same family and systematically improving the pharmacokinetic properties of the compound while maintaining the efficient inhibitory activity to USP7.
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