11β-Methoxyestradiol explained

11β-Methoxyestradiol (11β-MeOE2; developmental code name RU-2504) is a synthetic steroidal estrogen which was never marketed.[1] [2] [3] It has about 86% of the relative binding affinity of estradiol for the estrogen receptor. 11β-MeOE2 is structurally related to moxestrol (11β-methoxy-17α-ethynylestradiol). 11β-MeOE2 and moxestrol are substantially more potent than their non-methoxylated analogues (estradiol and ethinylestradiol, respectively) in mice.

See also

Notes and References

  1. Wolohan P, Reichert DE . CoMSIA and docking study of rhenium based estrogen receptor ligand analogs . Steroids . 72 . 3 . 247–260 . March 2007 . 17280694 . 1964785 . 10.1016/j.steroids.2006.11.011 .
  2. Katzenellenbogen JA, Muthyala R . Interactions of exogenous endocrine active substances with nuclear receptors. Pure and Applied Chemistry. 75. 11–12. 2003. 1797–1817. 1365-3075. 10.1351/pac200375111797. 86680540. free.
  3. Azadian-Boulanger G, Bertin D . Synthèse et activité utérotrophique des 11β-méthoxy estradiol 11β-méthoxy estriol et 11β-méthoxy 17α-éthynyl estradiol . Synthesis and uterotropic activity of 11β-methoxyestradiol, 11β-methoxyestriol, and 11β-methoxy-17α-ethynylestradiol . Chimica Therapeutica . 1973 . 8 . 4 . 451–454 . 0009-4374 . The prepn. and estrogenic activity of the 11β-methoxylated derivs. of estradiol, estriol, and 17α-ethynylestradiol were described. When administered orally to mice, the 3 compds. were from 10 to 1000 times more active than the corresponding nonmethoxylated estrogens..

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