Discovery of an Orally-Active Nonsteroidal Androgen Receptor Pure Antagonist and the Structure-Activity Relationships of Its Derivatives

Abstract

The 3-(4-cyano-3-trifluoromethylphenyl)-5,5-dimethylthiohydantoin derivatives which have carboxy-terminal side chains were synthesized and their agonistic/antagonistic activities against androgen receptor (AR) measured. Among them, compound 13b showed antagonistic activity (IC_<50>=130nm) with no agonistic activity even at 10000nm. This compound exhibited significant metabolic stability and oral antiandrogenic activity (ED_<50>=7mg/kg).

Journal

Chemical & pharmaceutical bulletin   [List of Volumes]

Chemical & pharmaceutical bulletin 56(11), 1555-1561, 2008-11-01  [Table of Contents]

The Pharmaceutical Society of Japan

References:  21

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Codes

  • NII Article ID (NAID) :
    110006968056
  • NII NACSIS-CAT ID (NCID) :
    AA00602100
  • Text Lang :
    ENG
  • Article Type :
    ART
  • ISSN :
    00092363
  • NDL Article ID :
    9685509
  • NDL Source Classification :
    ZS51(科学技術--薬学) // ZP1(科学技術--化学・化学工業)
  • NDL Call No. :
    Z53-D167
  • DOI :
    10.1248/cpb.56.1555
  • Databases :
    CJP  NDL  NII-ELS  J-STAGE 

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