http://www.cnr.it/ontology/cnr/individuo/prodotto/ID287992
A New Avenue toward Androgen Receptor Pan-antagonists: C2 Sterically Hindered Substitution of Hydroxy-propanamides (Articolo in rivista)
- Type
- Label
- A New Avenue toward Androgen Receptor Pan-antagonists: C2 Sterically Hindered Substitution of Hydroxy-propanamides (Articolo in rivista) (literal)
- Anno
- 2014-01-01T00:00:00+01:00 (literal)
- Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi
- 10.1021/jm5005122 (literal)
- Alternative label
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 (2014)
A New Avenue toward Androgen Receptor Pan-antagonists: C2 Sterically Hindered Substitution of Hydroxy-propanamides
in Journal of medicinal chemistry
(literal)
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- 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 (literal)
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- ISI Web of Science (WOS) (literal)
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- Italian National Research Council- Institute of Organic Synthesis and Photoreactivity;
Istituto Scientifico Romagnolo per lo Studio e la Cura dei Tumori;
Seconda Universita degli Studi di Napoli;
Istituto Regina Elena Roma;
Fondazione IRCCS Istituto Nazionale Tumori Milano (literal)
- Titolo
- A New Avenue toward Androgen Receptor Pan-antagonists: C2 Sterically Hindered Substitution of Hydroxy-propanamides (literal)
- Abstract
- 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 C2-substituted bicalutamide analogues to be obtained. Biological and theoretical evaluations demonstrate that C2-substitution with benzyl and phenyl moieties is a new, valuable option toward improving pan-antagonist behavior. Among the synthesized compounds, (R)-16m, when compared to casodex, (R)-bicalutamide, and enzalutamide, displayed very promising in vitro activity toward five different prostate cancer cell lines, all representative of CPRC and AIPC typical mutations. Despite being less active than (R)-bicalutamide, (R)-16m also displayed marked in vivo antitumor activity on VCaP xenografts and thus it may serve as starting point for developing novel AR pan-antagonists. (literal)
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