Synthesis and Structure–Activity Relationships of the First Ferrocenyl-Aryl-Hydantoin Derivatives of the Nonsteroidal Antiandrogen Nilutamide

    February 2008 in “ Journal of Medicinal Chemistry ”
    Olivier Payen, Siden Top, Anne Vessières, Emilie Brulé, Marie-Aude Plamont, Michael J. McGlinchey, Helge Müller-Bunz, Gérard Jaouen
    Image of study
    TLDR Scientists made the first metal-based compounds from a nonsteroidal antiandrogen drug, which showed potential in fighting both hormone-dependent and independent prostate cancer cells.
    In 2008, researchers synthesized the first organometallic complexes derived from the nonsteroidal antiandrogen nilutamide, with a ferrocenyl substituent. The N-substituted complexes had a weak or moderate antiproliferative effect (IC50 around 68 μM) on hormone-dependent and -independent prostate cancer cells. However, the C(5)-substituted compounds showed toxicity levels 10 times higher (IC50 around 5.4 µM), likely due to a structural effect linked to the aromatic character of the ferrocene. This effect seemed connected to a cytotoxic effect rather than an antihormonal one. The study suggested a new family of molecules that could be active against both hormone-dependent and hormone-independent prostate cancer cells.
    Discuss this study in the Community →

    Research cited in this study

    3 / 3 results

    Related Community Posts Join

    6 / 13 results

      community RU-58841 Lung Disease Possibility | Chest pain, "heart issues", etc

      in Treatment  24 upvotes 8 months ago
      Some users of RU-58841 report cardiovascular symptoms like heart palpitations and chest tightness, which may be linked to its metabolites causing lung disease. The safety of RU-58841 is uncertain due to lack of long-term data and concerns about product purity, especially from gray market sources.

      community So we’re just ok with taking a research chemical now?

      in Treatment  181 upvotes 3 years ago
      The conversation discusses the use of RU58841, a non-FDA approved research chemical for hair loss, with mixed opinions on its safety and effectiveness. Some users are willing to try it as a last resort after other treatments like Minoxidil and Finasteride failed, while others express concerns about potential long-term side effects and lack of official research.

      community For those on TRT and suffer from a more aggressive type of (AGA) hairloss, what are your hair safe protocols?

      in Chat  6 upvotes 1 year ago
      People on testosterone replacement therapy (TRT) with aggressive androgenetic alopecia (AGA) discuss using Dutasteride or Finasteride, sometimes combined with topical treatments like RU58841 or CB-03-01 (Breezula), to prevent hair loss. Concerns about side effects and costs of certain treatments are mentioned, with one individual sharing their experience of slowed hair loss using Finasteride alone.

      community Brutal... RU58841 , is that true ?

      in Update  162 upvotes 5 months ago
      The conversation discusses hair loss treatments, specifically Minoxidil, finasteride, and RU58841. Concerns are raised about the lack of studies on RU58841 and its potential effects.

      community Update: Chest discomfort from RU58841

      in Update  34 upvotes 9 months ago
      A user experienced severe chest pains and shortness of breath after using RU58841 for hair loss and was advised by a doctor that blocking androgens can weaken the heart. They decided to continue with finasteride, minoxidil, and a hair transplant instead.

    Similar Research

    5 / 68 results