Molecular Interactions of Progesterone Derivatives with 5α-Reductase Types 1 and 2 and Androgen Receptors

    March 2010 in “ Steroids ”
    Eugene Bratoeff, Perla García, Yvonne Heuze, Juan Soriano, Adriana Mejía, Ana María Labastida, Norma Valencia, Marisa Cabeza
    TLDR Certain progesterone derivatives can inhibit enzymes and reduce androgenic activity, potentially affecting prostate growth.
    The study investigated the molecular interactions of various progesterone derivatives with 5α-reductase types 1 and 2 and androgen receptors. Compounds 4 and 5 inhibited both isozymes, while compound 6 inhibited only type 1. Compounds 7a and 7b, with a chlorine or bromine atom at C-4, inhibited both isozymes, and their esterified forms (8a and 8b) inhibited only type 2. The study found that increased electronegativity in ring A enhanced inhibitory activity for type 1 but not type 2. Compounds 4, 5, 7a, and 7b bound to the androgen receptor, with 5 and 7b reducing prostate and seminal vesicle growth. The study highlighted the potential of these derivatives in modulating androgenic activity, although their IC50 values were higher compared to finasteride.
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