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- W1965843957 abstract "Eleven novel naftopidil-related compounds that contain amide and indole groups were designed and synthesized. The biological effects of these compounds on three α1-adrenoceptor subtypes and cancerous human prostate cell lines (PC-3, DU-145, and LNCaP) were determined. Compounds 2, 3, 5, 11, and 12 exhibited an α1-adrenoceptor antagonistic activity, whereas compounds 9, 10, and 12 displayed moderate antiproliferative activities. Compound 3 exhibited a significant α1D/1A blocking activity in isolated rat tissues (97.7- and 64.6-fold selective for α1D and α1A compared with α1B) but not a relevant cytotoxic activity. Compound 12 demonstrated a potent and selective α1D/1A antagonistic activity (47.9- and 19.1-fold for α1D and α1A compared with α1B) and a potent antiproliferative activity in PC-3 cells (IC50 = 15.70 μM). Further testing confirmed that compound 12 inhibited the growth of PC-3 cells by inducing apoptosis and G0/G1 cell cycle arrest, which was mediated by α1-adrenoceptor. Therefore, compound 12 is a potential multipotent agent that can act as an effective α1-adrenoceptor subtype antagonist for treating benign prostatic hyperplasia and a preventive medication against human prostate cancer." @default.
- W1965843957 created "2016-06-24" @default.
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- W1965843957 date "2015-05-01" @default.
- W1965843957 modified "2023-10-17" @default.
- W1965843957 title "Novel naftopidil-related derivatives and their biological effects as alpha1-adrenoceptors antagonists and antiproliferative agents" @default.
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- W1965843957 doi "https://doi.org/10.1016/j.ejmech.2015.04.005" @default.
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