452912-13-9Relevant academic research and scientific papers
Biphenyls as surrogates of the steroidal backbone. Part 2: Discovery of a novel family of non-steroidal 5-α-reductase inhibitors
Lesuisse, Dominique,Gourvest, Jean-Fran?ois,Albert, Eva,Doucet, Bernard,Hartmann, Catherine,Lefran?ois, Jean-Michel,Tessier, Sophie,Tric, Bernadette,Teutsch, Georges
, p. 1713 - 1716 (2007/10/03)
A new family of non-steroidal 5-α-reductase inhibitors was designed by replacing the steroid skeleton of an inhibitor related to estrone by a biphenyl moiety. This hypothesis originated from the reported estrogenic activity of a few biphenyl compounds (see Part 1 of this paper; Lesuisse et al. Bioorg. Med. Chem. Lett. 2001, 11, 1709). Two compounds turned out to be potent type 2 5-α-reductase inhibitors with IC50's of inhibition in the nanomolar range. These are to our knowledge amongst the most potent non-steroidal 5-α-reductase inhibitors described to date.
