Activity of Steroid 4 and Derivatives 4a–4f as Inhibitors of the Enzyme 5α-Reductase Type 1

    June 2018 in “ Bioorganic & medicinal chemistry ”
    Yazmín Arellano, Eugene Bratoeff, Yvonne Heuze, Marisol Bravo, Juan Soriano, Marisa Cabeza
    TLDR Compounds 4, 4b, and 4c effectively inhibit an enzyme linked to testosterone conversion without significant toxicity.
    The study synthesized and tested seven steroid derivatives (4, 4a–4f) as inhibitors of the enzyme 5α-reductase type 1 (5α-R1), which is predominant in metastatic prostate bone tumors. In vitro assays showed that compounds 4, 4b, and 4c effectively inhibited 5α-R1 activity. In vivo experiments on gonadectomized hamsters demonstrated that these derivatives reduced the diameter of flank glands and the weight of prostate and seminal vesicles without significant toxicity. The derivatives exhibited improved plasma half-life due to their stability against hydrolysis, with compound 4e showing the greatest pharmacological effect. The study concluded that these derivatives could serve as potential prodrugs for treating metastatic prostate cancer.
    Discuss this study in the Community →

    Research cited in this study

    1 / 1 results

    Related Community Posts Join

    6 / 484 results

      community 11 month progress on a cocktail regiment

      in Progress Pictures  440 upvotes 1 year ago
      The user "Dismal_Library_2264" shared their 11-month progress on a hair loss treatment regimen. They used dutasteride, topical minoxidil, dermarolling, a hair serum, and specific shampoos. They experienced some side effects but were overall satisfied with the results.

      community Nandrolone Replacement Therapy

      in Treatment  41 upvotes 1 year ago
      A user discusses starting nandrolone replacement therapy to stop hair loss and improve hair health, noting its benefits over finasteride. They report halted hair loss, improved skin, increased muscle, and a calm mood after three weeks.

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

      in Satire  7 upvotes 1 month 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.

      community How to know if shedding is from tren or minoxidil?

      in Minoxidil  5 upvotes 7 months ago
      The user started using trenbolone and minoxidil simultaneously and experienced increased hair shedding, unsure which is causing it. Replies suggest both drugs could cause hair loss, with one advising to stop trenbolone to protect hair and another indicating minoxidil is unlikely the cause due to the timing.

      community "but it will hurt my gains bro"

      in Satire  1302 upvotes 2 months ago
      The conversation humorously discusses hair loss treatments like Minoxidil, Finasteride, and Dutasteride, and their effects on hair and muscle gains. Users debate effectiveness and side effects, mixing scientific approaches with jokes.

    Similar Research

    5 / 1000+ results