Design, Synthesis, and Biological Evaluation of Chromone Derivatives as STAT1 Inhibitors for Treatment of Nonalcoholic Steatohepatitis

Zhipeng Zhang, Hongyan Lai, Shaofang Tian, Yingjie Song, Cunwuliji Na, Xiang Shi, Changhong He, Liuye Shi, Shengyun Wang, Fawad Ali, Fu Shu, Baoshun Zhang

Journal:JOURNAL OF MEDICINAL CHEMISTRY

IF:6.8

DOI:10.1021/acs.jmedchem.5c02431

PMID:41589317

Published:2026-01-27

research field:农学植物生物学分子遗传学

Abstract

Nonalcoholic steatohepatitis (NASH) is a chronic liver disease with a high global incidence rate, intricately linked to metabolic disorders. It is characterized by steatosis, inflammation, and hepatocyte ballooning. STAT1 is a transcription factor involved in metabolic regulation and progression of inflammatory responses. In this study, we have identified STAT1 as a novel therapeutic target for NASH. Using our established STAT1 inhibitor screening platform, we identified the compound ZDZ-553, which is characterized by a chromone skeleton, demonstrates potent inhibitory activity against STAT1, and exhibits a favorable safety profile. In the NASH mouse model experiment, ZDZ-553 significantly ameliorated liver steatosis and inflammatory responses. These findings collectively suggest that ZDZ-553 could be a promising candidate for treatment of NASH, highlighting the therapeutic potential of targeting STAT1.

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