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 journalArticle

7 Citations (Scopus)

Abstract

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
Pages (from-to)454-458
Number of pages5
JournalACS Medicinal Chemistry Letters
Volume3
Issue number6
DOIs
Publication statusPublished - May 14 2012

Fingerprint

Androgen Receptors
Nitrogen
Ligands
Androgen Antagonists
Disclosure
Oxygen
Derivatives
bicalutamide

Keywords

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

ASJC Scopus subject areas

  • Organic Chemistry
  • Drug Discovery
  • Biochemistry

Cite this

Varchi, G., Guerrini, A., Tesei, A., Brigliadori, G., Bertucci, C., Di Donato, M., & Castoria, G. (2012). Nonsteroidal androgen receptor ligands: Versatile syntheses and biological data. ACS Medicinal Chemistry Letters, 3(6), 454-458. https://doi.org/10.1021/ml3000269

Nonsteroidal androgen receptor ligands : Versatile syntheses and biological data. / Varchi, Greta; Guerrini, Andrea; Tesei, Anna; Brigliadori, Giovanni; Bertucci, Carlo; Di Donato, Marzia; Castoria, Gabriella.

In: ACS Medicinal Chemistry Letters, Vol. 3, No. 6, 14.05.2012, p. 454-458.

Research output: Contribution to journalArticle

Varchi, G, Guerrini, A, Tesei, A, Brigliadori, G, Bertucci, C, Di Donato, M & Castoria, G 2012, 'Nonsteroidal androgen receptor ligands: Versatile syntheses and biological data', ACS Medicinal Chemistry Letters, vol. 3, no. 6, pp. 454-458. https://doi.org/10.1021/ml3000269
Varchi, Greta ; Guerrini, Andrea ; Tesei, Anna ; Brigliadori, Giovanni ; Bertucci, Carlo ; Di Donato, Marzia ; Castoria, Gabriella. / Nonsteroidal androgen receptor ligands : Versatile syntheses and biological data. In: ACS Medicinal Chemistry Letters. 2012 ; Vol. 3, No. 6. pp. 454-458.
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