Synthesis and Biological Evaluation of Esters of 16-Formyl-17-Methoxy-Dehydroepiandrosterone Derivatives as Inhibitors of 5α-Reductase Type 2

    November 2015 in “ Journal of Enzyme Inhibition and Medicinal Chemistry ”
    Araceli Sánchez‐Márquez, Yazmín Arellano, Eugene Bratoeff, Yvonne Heuze, Karen Córdova, Gladys Nieves, Juan Soriano, Marisa Cabeza
    TLDR Certain derivatives are more effective 5α-reductase type 2 inhibitors than finasteride.
    This study investigated the inhibitory effects of 16-formyl-17-methoxy-dehydroepiandrosterone derivatives on 5α-reductase type 2 (5α-R2) using human prostate tissue. The derivatives with aliphatic ester moieties at the C-3 position were found to be more potent than finasteride, a known 5α-R2 inhibitor, due to increased lipophilicity. Compounds 5a–5d, particularly 5b, showed significantly higher potency, with 5b being 200 times more effective than finasteride. The derivatives did not bind to androgen receptors, suggesting they do not compete with natural ligands. The study suggested these compounds could be developed as prodrugs for conditions like androgenetic alopecia and prostate cancer, with potential reduced toxicity due to ester masking of the toxic formyl group. The compounds were non-toxic in hamster models, supporting further investigation.
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      in Research/Science  43 upvotes 1 week ago
      Minoxidil is not an anti-androgen; it is a growth stimulator and does not lower DHT like finasteride or dutasteride. Minoxidil can cause side effects like facial swelling and anxiety due to its vasodilator properties.

      community Having androgen receptor density and sensitivity at wrong f*ing place

      in Satire  7 upvotes 1 year ago
      The conversation discusses hair loss treatments, focusing on the use of topical minoxidil, microneedling, finasteride, and dutasteride, while debating the role of testosterone and DHT in hair loss. It also touches on the potential liver health impacts of these treatments and the genetic sensitivity of hair follicles to androgens.

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      in Research/Science  323 upvotes 1 month ago
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