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Letters in Drug Design & Discovery

Volume 8 Issue 5
ISSN: 1570-1808
eISSN: 1875-628X

 

   All Titles

  Synthesis and Biological Evaluation of Spiro-δ-lactones as Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 2 (17β-HSD2)
  pp.406-421 (16) Authors: Kuiying Xu, Marie Wetzel, Rolf W. Hartmann, Sandrine Marchais-Oberwinkler
 
 
      Abstract

17β-Hydroxysteroid dehydrogenase type 2 (17β-HSD2) catalyzes the oxidation of the potent estradiol (E2) to the less active estrogen estrone (E1). Inhibitors of this enzyme should maintain the local level of E2 in bone tissue when the E2 concentration in the circulation drops and therefore might be useful for the treatment of osteoporosis. In this work, novel non-steroidal spiro-δ-lactone compounds designed as 17β-HSD2 inhibitors were synthesized and their physicochemical and biological properties were investigated. These new spiro-δ-lactones are not sufficiently stable for further development and show low inhibition of the enzyme.

 
  Keywords: 17β-hydroxysteroid dehydrogenase type 2 inhibitors, Drug design, Osteoporosis, Spiro-δ-lactones, Steroidomimetics, Biological Evaluation, Spiro-lactones, Inhibitors, 17-Hydroxysteroid, Dehydrogenase, SDRs, dihydrotestosterone, 4-androstene-3,17-dione, spirolactone derivatives, aromatase inhibitors
  Affiliation: Pharmaceutical and Medicinal Chemistry, Saarland University, Campus C23, D-66123Saarbrucken, Germany.
 
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