Raloxifene-driven benzothiophene derivatives: Discovery, structural refinement, and biological evaluation as potent PPARγ modulators based on drug repurposing

Liu, Qingmei; Ma, Lei; Chen, Fangyuan; Zhang, Shuyun; Huang, Zexin; Zheng, Xiufen; Chen, Zikai; Ye, Junwei; Hou, Ning; Yi, Wei; Zhou, Zhi

doi:10.1016/j.ejmech.2024.116325

European Journal of Medicinal Chemistry

2024

DOI: 10.1016/j.ejmech.2024.116325

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Raloxifene-driven benzothiophene derivatives: Discovery, structural refinement, and biological evaluation as potent PPARγ modulators based on drug repurposing

Qingmei Liu,

Lei Ma,

Fangyuan Chen

et al.

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Cited by 2 publications

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Structure-based screening, optimization and biological evaluation of novel chrysin-based derivatives as selective PPARγ modulators for the treatment of T2DM and hepatic steatosis

Ma,

Tang,

Chen

et al. 2024

European Journal of Medicinal Chemistry

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Structure-based screening, optimization and biological evaluation of novel chrysin-based derivatives as selective PPARγ modulators for the treatment of T2DM and hepatic steatosis

Ma,

Tang,

Chen

et al. 2024

European Journal of Medicinal Chemistry

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An Overview of the Pharmacological Activities and Synthesis of Benzothiophene Derivatives

Pathak,

Singh,

Sharma

et al. 2024

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One important class of organic compounds having many uses, especially in medical chemistry, is benzothiophene and its derivatives. This review examines the biological activity of benzothiophene derivatives and summarizes the synthetic methods used in their production. The effectiveness of several synthetic pathways, such as cyclization techniques, functional group modifications, and reactions catalyzed by transition metals, in gaining access to benzothiophene scaffolds has been examined. Additionally, a broad spectrum of therapeutic domains, such as antiinflammatory, antibacterial, antidiabetic, anticancer, antimicrobial, anti-leishmanial, antifungal, antimalarial, and antitubercular activities, are covered by the pharmacological activities that are being explored. The synthesis and pharmacological potential of benzothiophene derivatives are well-explained in this thorough review, which opens up new options for medicinal chemistry and drug discovery study. Overall, this study is a useful resource for scientists working on drug development and discovery as it sheds light on the pharmacological potential of benzothiophene derivatives. This review includes the synthesis and bioactivities of the years 2002-2024. The goal of this review is to compile the existing information on benzothiophene derivatives and provide guidance for future research and development as well as insights into their possible medicinal uses.

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Raloxifene-driven benzothiophene derivatives: Discovery, structural refinement, and biological evaluation as potent PPARγ modulators based on drug repurposing

Cited by 2 publications

References 60 publications

Structure-based screening, optimization and biological evaluation of novel chrysin-based derivatives as selective PPARγ modulators for the treatment of T2DM and hepatic steatosis

Structure-based screening, optimization and biological evaluation of novel chrysin-based derivatives as selective PPARγ modulators for the treatment of T2DM and hepatic steatosis

An Overview of the Pharmacological Activities and Synthesis of Benzothiophene Derivatives

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