Novel Heterocyclic Pyrimidine Derivatives as GSK3α Inhibitors

IF 3.5 3区医学 Q2 CHEMISTRY, MEDICINAL

ACS Medicinal Chemistry Letters Pub Date : 2025-04-07 DOI:10.1021/acsmedchemlett.5c0015910.1021/acsmedchemlett.5c00159

Yinlong Li, and , Steven H. Liang*,

引用次数: 0

Abstract

This patent highlight describes a series of novel heterocyclic pyrimidine derivatives as glycogen synthase kinase 3 alpha (GSK3α) inhibitors. The disclosed compounds demonstrated excellent subtype selectivity over GSK3β and showed promising efficacy in treating an MC38 mouse model of colorectal cancer.

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新型杂环嘧啶衍生物作为GSK3α抑制剂

本专利重点描述了一系列新的杂环嘧啶衍生物作为糖原合成酶激酶3α (GSK3α)抑制剂。所披露的化合物对GSK3β具有良好的亚型选择性，在MC38小鼠结直肠癌模型中显示出良好的疗效。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

ACS Medicinal Chemistry Letters CHEMISTRY, MEDICINAL-

CiteScore

7.30

自引率

2.40%

发文量

328

审稿时长

1 months

期刊介绍： ACS Medicinal Chemistry Letters is interested in receiving manuscripts that discuss various aspects of medicinal chemistry. The journal will publish studies that pertain to a broad range of subject matter, including compound design and optimization, biological evaluation, drug delivery, imaging agents, and pharmacology of both small and large bioactive molecules. Specific areas include but are not limited to: Identification, synthesis, and optimization of lead biologically active molecules and drugs (small molecules and biologics) Biological characterization of new molecular entities in the context of drug discovery Computational, cheminformatics, and structural studies for the identification or SAR analysis of bioactive molecules, ligands and their targets, etc. Novel and improved methodologies, including radiation biochemistry, with broad application to medicinal chemistry Discovery technologies for biologically active molecules from both synthetic and natural (plant and other) sources Pharmacokinetic/pharmacodynamic studies that address mechanisms underlying drug disposition and response Pharmacogenetic and pharmacogenomic studies used to enhance drug design and the translation of medicinal chemistry into the clinic Mechanistic drug metabolism and regulation of metabolic enzyme gene expression Chemistry patents relevant to the medicinal chemistry field.