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
    Image of study
    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.
    Discuss this study in the Community →

    Related Community Posts Join

    6 / 1000+ results

      community Why is Kevin Mann (Haircafe) Hated?

      in Chat  62 upvotes 1 year ago
      Hair loss treatments, including microneedling, minoxidil, finasteride and RU58841; the efficacy of these treatments; criticisms of Kevin Mann's content related to his selective data presentation and biases towards certain treatments; and other topics such as DHT being labeled a "trash hormone" and critiques of other hairloss YouTubers.

      community Does CosmeRNA target the root cause of MPB?

      in Chat 1 year ago
      . CumsOnYourFeet69 has been discussing a new treatment called CosmeRNA which claims to target the root cause of male pattern baldness, and is considering using it in conjunction with Minoxidil instead of Finasteride due to possible side effects. Replies have highlighted that the efficacy of this treatment is still unknown, but it could be used as an effective maintenance option if successful.

      community KX-826: Long-Term Safety Results are out!

      in Research/Science  158 upvotes 1 month ago
      KX-826 initially improves hair growth but declines after 24 weeks, with mild itching as a side effect. Combining it with minoxidil and finasteride may improve results, but long-term effectiveness is uncertain.

    Similar Research

    5 / 1000+ results