Doxazosin-related alpha1-adrenoceptor antagonists with prostate antitumor activity.
J Med Chem
; 52(15): 4951-4, 2009 Aug 13.
Article
en En
| MEDLINE
| ID: mdl-19719240
ABSTRACT
Doxazosin analogues 1-3 and 1a were synthesized and investigated at alpha1-adrenoceptors and PC-3, DU-145, and LNCaP human prostate cancer cells. Compound 1 (cyclodoxazosin) was a potent alpha(1B)-adrenoceptor antagonist displaying antiproliferative activity higher than that of doxazosin in cancer cells in vitro and in vivo, respectively. Because of its antitumor efficacy at low concentrations, lower apoptotic activity in NHDF vs tumor cells, and antiangiogenetic effect, 1 showed a better therapeutic profile relative to doxazosin.
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Neoplasias de la Próstata
/
Doxazosina
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Antagonistas Adrenérgicos alfa
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Antagonistas de Receptores Adrenérgicos alfa 1
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Antineoplásicos
Límite:
Animals
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Humans
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Male
Idioma:
En
Revista:
J Med Chem
Asunto de la revista:
QUIMICA
Año:
2009
Tipo del documento:
Article
País de afiliación:
Italia