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Nonsteroidal androgen receptor ligands: versatile syntheses and biological data.


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.

SUBMITTER: Varchi G 

PROVIDER: S-EPMC4025740 | biostudies-literature | 2012 Jun

REPOSITORIES: biostudies-literature

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Nonsteroidal androgen receptor ligands: versatile syntheses and biological data.

Varchi Greta G   Guerrini Andrea A   Tesei Anna A   Brigliadori Giovanni G   Bertucci Carlo C   Di Donato Marzia M   Castoria Gabriella G  

ACS medicinal chemistry letters 20120410 6


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. ...[more]

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