Nonsteroidal androgen receptor ligands: Versatile syntheses and biological data

Greta Varchi, Andrea Guerrini, Anna Tesei, Giovanni Brigliadori, Carlo Bertucci, Marzia Di Donato, Gabriella Castoria

Research output: Contribution to journalArticlepeer-review

9 Scopus citations


We report herein a stereoselective and straightforward methodology for the synthesis of new androgen receptor ligands with (anti)-agonistic activities. Oxygen-nitrogen replacement in bicalutamide-like structures paves the way to the disclosure of a new class of analogues, including cyclized/nitrogen-substituted derivatives, with promising antiandrogen (or anabolic) activity.

Original languageEnglish (US)
Pages (from-to)454-458
Number of pages5
JournalACS Medicinal Chemistry Letters
Issue number6
StatePublished - May 14 2012


  • androgen receptor
  • enantiopure antiandrogens
  • hormone-refractory prostate cancer
  • sulfinylimino propanamides

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry


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