Synthesis, Biological Evaluation, and Molecular Docking of 4-Amino-2H-benzo[h]chromen-2-one Analogs Containing the Piperazine Moiety

    August 2019 in “ Bioorganic & medicinal chemistry ”
    Hong Chen, Jingxiao Zhang, Pu-Zhou Hu, Yuna Qian, Jing Li, Jianliang Shen
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    TLDR Analog 23 is a promising compound for prostate cancer treatment.
    Researchers designed and synthesized 22 analogs of 4-Amino-2H-benzo[h]chromen-2-one as potential anti-prostate cancer agents targeting androgen receptors (AR). Thirteen analogs (3, 4, 5, 7, 8, 10, 11, 12, 16, 18, 21, 23, and 24) showed significant AR antagonistic activity (inhibition >50%) and higher efficacy than finasteride in AR-rich LNCaP cells compared to AR-deficient PC-3 cells. Molecular docking indicated that the most potent compound, analog 23, binds to the AR ligand binding pocket via Van der Waals interactions. This study provided a promising lead compound for prostate cancer therapy and advanced the development of novel AR antagonists.
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