Synthesis, Characterization and Evaluation of 5α, 6β-Dihalo Androsterone Derivatives as 5α-Reductase Inhibitors

    May 2022 in “ Current Enzyme Inhibition ”
    Akanksha Sharma, Priyanka S. Rana, Poonam Arora, Tanzeer Kaur, Neelima Dhingra
    TLDR Compound 7b is a promising candidate for treating benign prostatic hyperplasia and prostate cancer.
    The study synthesized and characterized a series of 5α, 6β-Dichloro-17-Oxoandrostan-3β-yl esters (7a-7f) to evaluate their 5α-reductase inhibitory activity. The compounds demonstrated increased anti-androgenic activity compared to finasteride, with compound 7b showing the highest inhibitory activity and improved solubility and dissolution properties. These findings suggest that the presence of an electronegative group at position 3 enhances the activity, making compound 7b a promising candidate for further development and formulation against benign prostatic hyperplasia and prostate cancer.
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