Design, Synthesis and Anti-Tumor Evaluation of Novel Thiohydantoin Congeners as Androgen Receptor Antagonists With In Vivo Study

    May 2024 in “ Journal of molecular structure ”
    Nada M. Mohamed, Shaimaa I. El Rabeeb, Moshira A. El Deeb, Amal M. Mahfoz, Fatma G. Abdulrahman
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    Studysummary This study found that a novel thiohydantoin derivative, 3a, effectively inhibited androgen receptor activity in LNCaP cells and showed promising in vivo results by reducing testosterone-induced prostate changes, outperforming finasteride in mitigating prostate index and histopathological alterations.
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    The study focused on designing and synthesizing novel thiohydantoin derivatives as androgen receptor antagonists to treat prostate cancer. The di-cyanide analogues 3a-b and 3d demonstrated significant growth inhibition of androgen-sensitive LNCaP cells with IC50 values ranging from 2.64 to 20.62 µM. Hydrolyzing one cyanide group to an amide maintained activity, while conversion to an ester reduced it. Hydrophobic substitutions on the phenyl moiety improved predicted logP and growth inhibition. The study was self-funded and conducted by the authors without external financial support.
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