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Design, Synthesis, Biological Evaluation, and Molecular Docking Studies of Thiazolidine-2,4-dione Derivatives as Mcl-1 Inhibitors

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Abstract

In the study, two series of thiazolidine-2,4-dione derivatives have been designed, synthesized and evaluated for their inhibitory activity of Mcl-1 protein by fluorescence polarization assays (FPAs). Among those, the most potent product has demonstrated inhibitory activity against Mcl-1 (inhibitory rate 94% at 10 μM) higher than that of the positive control WL-276 (90%).

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Funding

This work was supported by National Natural Science Foundation of China (Grant no. 82003602, 21877034), the science and technology innovation Program of Hunan Province (Grant no. 2021RC5028), Scientific Research Fund of Hunan Provincial Education Department (Grant no. 21B0478) and Open Project Program of Key Laboratory of Theoretical Organic Chemistry and Functional Molecule, Ministry of Education (Grant no. LKF202105).

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Authors and Affiliations

  1. Key Laboratory of Theoretical Organic Chemistry and Functional Molecule, Ministry of Education, School of Chemistry and Chemical Engineering, Hunan University of Science and Technology, Xiangtan, 411201, Hunan, China

    Xu Deng, Jiabing Long, Wenyan Wang, Shen Xia & Yichao Wan

  2. Hunan Provincial Key Laboratory of Controllable Preparation and Functional Application of Fine Polymers, Hunan Provincial Key Lab of Advanced Materials for New Energy Storage and Conversion, Hunan University of Science and Technology, Xiangtan, 411201, Hunan, China

    Yichao Wan

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  1. Xu Deng
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  2. Jiabing Long
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  3. Wenyan Wang
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  4. Shen Xia
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Correspondence to Yichao Wan.

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Deng, X., Long, J., Wang, W. et al. Design, Synthesis, Biological Evaluation, and Molecular Docking Studies of Thiazolidine-2,4-dione Derivatives as Mcl-1 Inhibitors. Russ J Gen Chem 92, 464–469 (2022). https://doi.org/10.1134/S1070363222030148

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  • DOI: https://doi.org/10.1134/S1070363222030148

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