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 alpha1B-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 anti-angiogenetic effect, 1 showed a better therapeutic profile relative to doxazosin.
Doxazosin-related alpha1-adrenoceptor antagonists with prostate antitumor activity
GIARDINA', Dario;SAGRATINI, Gianni;ANGELI, Piero;POMPEI, Pierluigi
2009-01-01
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 alpha1B-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 anti-angiogenetic effect, 1 showed a better therapeutic profile relative to doxazosin.File in questo prodotto:
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