Nonsteroidal androgen receptor ligands: Versatile syntheses and biological data

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

doi:10.1021/ml3000269

Nonsteroidal androgen receptor ligands: Versatile syntheses and biological data

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

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9 Scopus citations

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 language	English (US)
Pages (from-to)	454-458
Number of pages	5
Journal	ACS Medicinal Chemistry Letters
Volume	3
Issue number	6
DOIs	https://doi.org/10.1021/ml3000269
State	Published - May 14 2012

Keywords

androgen receptor
enantiopure antiandrogens
hormone-refractory prostate cancer
sulfinylimino propanamides

ASJC Scopus subject areas

Biochemistry
Drug Discovery
Organic Chemistry

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10.1021/ml3000269

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AU - Varchi, Greta

AU - Guerrini, Andrea

AU - Tesei, Anna

AU - Brigliadori, Giovanni

AU - Bertucci, Carlo

AU - Di Donato, Marzia

AU - Castoria, Gabriella

PY - 2012/5/14

Y1 - 2012/5/14

N2 - 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.

AB - 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.

KW - androgen receptor

KW - enantiopure antiandrogens

KW - hormone-refractory prostate cancer

KW - sulfinylimino propanamides

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ER -

Nonsteroidal androgen receptor ligands: Versatile syntheses and biological data

Abstract

Keywords

ASJC Scopus subject areas

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