Synthesis of Novel Androstane-N-Cyclohexyl-17-Carboxamides and Their Effect on 5α-Reductase Isoform 2, Androgen Receptor, and Androgen-Dependent Glands

    November 2021 in “ Pharmaceutical Sciences ”
    Juan Carlos Lopez-Lezama, Marisa Cabeza, Yvonne Heuze, Araceli Sánchez, José M. Rojas, Norma Angélica Valencia-Islas
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    TLDR New compounds were made and tested, with compound 6 showing potential for treating prostate-related diseases.
    The study aimed to synthesize and evaluate the biological activity of new compounds for the treatment of androgen-dependent diseases such as Benign Prostatic Hyperplasia (BPH) and Prostate Cancer (PCa). The researchers synthesized three compounds (6, 7, and 8) and tested their affinity to the androgen receptor (AR) and their inhibitory activity on the 5α-reductase isoform 2 (5RD5A2). Compound 6 showed higher potency as an inhibitor of 5RD5A2 compared to finasteride, a known inhibitor. It also reduced the weight of androgen-dependent glands such as the prostate. Compound 7 only decreased the diameter of flank organs, while compound 8 increased these parameters. The findings suggest that compound 6 could be a potential lead for new drugs to treat BPH and PCa.
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