1085928-20-6Relevant articles and documents
Novel naftopidil-related derivatives and their biological effects as alpha1-adrenoceptors antagonists and antiproliferative agents
Huang, Junjun,He, Fei,Huang, Minyi,Liu, Xiawen,Xiong, Yan,Huang, Yajian,Zhu, Liu,Yang, Ya,Xu, Xingjie,Yuan, Mu
, p. 83 - 91 (2015)
Eleven novel naftopidil-related compounds that contain amide and indole groups were designed and synthesized. The biological effects of these compounds on three ±1-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 1-adrenoceptor antagonistic activity, whereas compounds 9, 10, and 12 displayed moderate antiproliferative activities. Compound 3 exhibited a significant ±1D/1A blocking activity in isolated rat tissues (97.7-and 64.6-fold selective for ±1D and ±1A compared with 1B) but not a relevant cytotoxic activity. Compound 12 demonstrated a potent and selective 1D/1A antagonistic activity (47.9-and 19.1-fold for 1D and ±1A compared with ±1B) 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 ±1-adrenoceptor. Therefore, compound 12 is a potential multipotent agent that can act as an effective ±1-adrenoceptor subtype antagonist for treating benign prostatic hyperplasia and a preventive medication against human prostate cancer.
COMPSITIONS, SYNTHESIS, AND METHODS OF USING QUINOLINE BASED ATYPICAL ANTIPSYCHOTIC AGENTS
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Page/Page column 30, (2009/01/20)
The present invention provides novel quinolinone derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder, and depression.