Recent advances in small molecule design strategies against hepatic fibrosis

IF 5.9 2区 医学 Q1 CHEMISTRY, MEDICINAL European Journal of Medicinal Chemistry Pub Date : 2025-03-15 Epub Date: 2025-01-17 DOI:10.1016/j.ejmech.2025.117281
Heming Chen , Wei Su , Tingting Li , Yun Wang , Zhuangyu Li , Liyan Xiong , Zhe-Sheng Chen , Chuan Zhang , Tingfang Wang
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Abstract

Hepatic fibrosis, a widespread pathological process observed across various liver diseases, is acknowledged as a potentially reversible condition. In recent years, liver fibrosis has garnered extensive research attention, with a primary emphasis on developing drugs that can directly block or reverse this condition. This paper presents a comprehensive review of the design strategies for various anti-hepatic fibrosis agents that have been many efficacious small-molecule drugs. This review encompasses the synthesis and design of nuclear receptor ligands (such as VDR and Nurr7), kinase inhibitors (including ALK5 and JAK1), selective PDE inhibitors, small-molecule monomers derived from natural products, and other small molecules. The aim of this review is to provide promising avenues and valuable insights for the continued development of anti-hepatic fibrosis drugs.

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抗肝纤维化小分子设计策略的最新进展
肝纤维化是一种广泛存在于各种肝脏疾病中的病理过程,被认为是一种潜在的可逆性疾病。近年来,肝纤维化获得了广泛的研究关注,主要重点是开发可以直接阻断或逆转这种疾病的药物。本文综述了各种抗肝纤维化药物的设计策略,这些药物是许多有效的小分子药物。本文综述了核受体配体(如VDR和Nurr7)、激酶抑制剂(包括ALK5和JAK1)、选择性PDE抑制剂、天然产物衍生的小分子单体和其他小分子的合成和设计。本文综述的目的是为抗肝纤维化药物的持续开发提供有希望的途径和有价值的见解。
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来源期刊
CiteScore
11.70
自引率
9.00%
发文量
863
审稿时长
29 days
期刊介绍: The European Journal of Medicinal Chemistry is a global journal that publishes studies on all aspects of medicinal chemistry. It provides a medium for publication of original papers and also welcomes critical review papers. A typical paper would report on the organic synthesis, characterization and pharmacological evaluation of compounds. Other topics of interest are drug design, QSAR, molecular modeling, drug-receptor interactions, molecular aspects of drug metabolism, prodrug synthesis and drug targeting. The journal expects manuscripts to present the rational for a study, provide insight into the design of compounds or understanding of mechanism, or clarify the targets.
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