title: Biphenyls as surrogates of the steroidal backbone. Part 2: discovery of a novel family of non-steroidal 5-alpha-reductase inhibitors.
abstract: A new family of non-steroidal 5-alpha-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-alpha-reductase inhibitors with IC(50)'s of inhibition in the nanomolar range. These are to our knowledge amongst the most potent non-steroidal 5-alpha-reductase inhibitors described to date.
authors: Medicinal Chemistry, Aventis, 102 route de Noisy, 93235 Cedex, Romainville, France. dominique.lesuisse@aventis.com
authors: D
authors: D
authors: Lesuisse
authors: J F
authors: JF
authors: Gourvest
authors: E
authors: E
authors: Albert
authors: B
authors: B
authors: Doucet
authors: C
authors: C
authors: Hartmann
authors: J M
authors: JM
authors: Lefrançois
authors: S
authors: S
authors: Tessier
authors: B
authors: B
authors: Tric
authors: G
authors: G
authors: Teutsch
mesh_terms: D058891:5-alpha Reductase Inhibitors; D001713:Biphenyl Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D013256:Steroids / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D058891:5-alpha Reductase Inhibitors; D001713:Biphenyl Compounds; D004791:Enzyme Inhibitors; D013256:Steroids