Article
A new avenue toward androgen receptor pan-antagonists: C2 sterically hindered substitution of hydroxy-propanamides.
Journal of medicinal chemistry - 11 Sept 2014
Guerrini Andrea, Tesei Anna, Ferroni Claudia, Paganelli Giulia, Zamagni Alice, Carloni Silvia, Di Donato Marzia, Castoria Gabriella, Leonetti Carlo, Porru Manuela, De Cesare Michelandrea, Zaffaroni Nadia, Beretta Giovanni Luca, Del Rio Alberto, Varchi Greta
Abstract excerpt
The androgen receptor (AR) represents the primary target for prostate cancer (PC) treatment even when the disease progresses toward androgen-independent (AIPC) or castration-resistant (CRPC) forms. Because small chemical changes in the structure of nonsteroidal AR ligands determine the pharmacological responses of AR, we developed a novel stereoselective synthetic strategy that allows sterically hindered...
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