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Doxazosin-related alpha1-adrenoceptor antagonists with prostate antitumor activity. 2009
Dario Giardinà, and
Daniele Martarelli, and
Gianni Sagratini, and
Piero Angeli, and
Dario Ballinari, and
Ugo Gulini, and
Carlo Melchiorre, and
Elena Poggesi, and
Pierluigi Pompei
Department of Chemical Sciences, University of Camerino, Camerino, Italy. dario.giardina@unicam.it
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.
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