RU-57073

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RU-57073
RU-57073.svg
Clinical data
Drug classNonsteroidal antiandrogen
Identifiers
CAS Number
PubChem CID
Chemical and physical data
FormulaC15H14F3N3O2S
Molar mass357.351 g/mol g·mol−1
3D model (JSmol)

RU-57073 is a nonsteroidal antiandrogen which was never marketed.[1][2][3] It shows 163% of the affinity of testosterone for the androgen receptor and negligible affinity for other steroid hormone receptors.[1][2]

Affinities of a selection of androgen receptor
ligands at steroid hormone receptors

Compound AR ER PR GR MR
Metribolone 290 < 0.1 190 4 38
Dihydrotestosterone 180 ? ? ? ?
Testosterone 100 ? ? ? ?
Cyproterone acetate 10 ? ? ? ?
Bicalutamide 1.8 ? ? ? ?
Nilutamide 0.8 ? ? ? ?
Hydroxyflutamide 0.8 ? ? ? ?
RU-59063 300 <0.1 <0.1 <0.1 <0.1
RU-58841 150 ? ? ? ?
RU-58642 46 <0.1 <0.1 <0.1 <0.1
RU-57073 163 <0.1 <0.1 <0.1 <0.1
RU-56187 92 <0.1 <0.1 <0.1 <0.1
Notes: Values are RBAs (%). Reference ligands (100%) were testosterone for the AR, estradiol for the ERα and ERβ, progesterone for the PR, dexamethasone for the GR, and aldosterone for the MR. Sources: See template.

See also[edit]

References[edit]

  1. ^ a b Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): structure-activity relationships". Curr. Med. Chem. 7 (2): 211–47. doi:10.2174/0929867003375371. PMID 10637363.
  2. ^ a b Teutsch G, Goubet F, Battmann T, Bonfils A, Bouchoux F, Cerede E, Gofflo D, Gaillard-Kelly M, Philibert D (January 1994). "Non-steroidal antiandrogens: synthesis and biological profile of high-affinity ligands for the androgen receptor". J. Steroid Biochem. Mol. Biol. 48 (1): 111–9. doi:10.1016/0960-0760(94)90257-7. PMID 8136296.
  3. ^ Münster U, Nakamura C, Haberland A, Jores K, Mehnert W, Rummel S, Schaller M, Korting HC, Zouboulis CC, Blume-Peytavi U, Schäfer-Korting M (January 2005). "RU 58841-myristate--prodrug development for topical treatment of acne and androgenetic alopecia". Pharmazie. 60 (1): 8–12. PMID 15700772.