1,048
Views
5
CrossRef citations to date
0
Altmetric
Research Article

Synthesis and biological activity of progesterone derivatives as 5α-reductase inhibitors, and their effect on hamster prostate weight

, , , , &
Pages 306-311 | Received 18 Feb 2009, Accepted 08 Jun 2009, Published online: 29 Oct 2009

References

  • Luu-The V, Bélanger A, Labrie F. Androgen biosynthetic pathways in human prostate. Best Pract Res Clin Endocrinol Metab 2008;22:207–21.
  • Krieg M, Weiser H, Tunn S. Potential activities of androgen metabolizing enzymes in human prostate. J Steroid Biochem Mol Biol 1995;53:395–400.
  • Bratoeff E, Ramírez E, Flores E, Sánchez M, Heuze I, Cabeza M. New aromatic esters of progesterone as antiandrogens. J Enzyme Inhib Med Chem 2004;19:99–105.
  • Anderson KM, Liao S. Selective retention of dihydrotestosterone by prostatic nuclei. Nature 1968;219:277–9.
  • Russell DW, Wilson JD. Steroid 5α-reductase: two genes/two enzymes. Annu Rev Biochem 1994;63:25–61.
  • Machetti F, Guarna A. Novel inhibitors of 5α-reductase. Expert Opin Ther Patents 2002;12:201–15.
  • Flores E, Bratoeff E, Cabeza M, Ramírez E, Quiroz A, Heuze I. Steroid 5α-reductase inhibitors. Mini Rev Med Chem 2003;3:225–37.
  • Bratoeff E, Carrillo E, Magaña M. Synthesis of 4 and 6-halopregnadiene derivatives with antiandrogenic activity. Mex Pharm Soc 1991;21:25–9.
  • Hendry PWJ, Danzo BJ. Structural conversion of cytosolic steroid receptors by an age-dependent epididymal protease. J Steroid Biochem 1985;21:883–93.
  • Liang T, Heiss EJ. Inhibition of 5α-reductase, receptor binding, and nuclear uptake of androgens in the prostate by a 4-methyl-4-aza-steroid. Biol Chem 1981;256:7998–8005.
  • Bradford MM. A rapid and sensitive method for the quantization of micrograms quantities of protein utilizing the principle of protein dye binding. Anal Biochem 1986;72:248–54.
  • Hirosumi J, Nakayama O, Fagan T, Sawada K, Chida N, Inami M, et al. FK143, a novel non steroidal inhibition of steroid 5α-reductase: in vitro effects of human and animal prostatic enzymes. J Steroid Biochem Mol Biol 1995;52:357–63.
  • Bratoeff E, Cabeza M, Pérez-Ornelas V, Recillas S, Heuze I. In vivo and in vitro effect of novel 4, 16-pregnadiene-6, 20 dione derivatives, as 5α-reductase inhibitors. J Steroid Biochem Mol Biol 2008;111:275–81.
  • Cabeza M, Vilchis F, Lemus A, Díaz de León L, Pérez-Palacios G. Molecular interactions of levonorgestrel and its 5α-reduced derivative with androgen receptors in hamster flanking organs. Steroids 1995;60:630–5.
  • Pérez-Ornbelas V, Cabeza M, Bratoeff E, Heuze I, Sánchez M, Ramírez E, et al. New 5α-reductase inhibitors: in vitro and in vivo effects. Steroids 2005;70:217–24.

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.