Synthesis, biological evaluation and SAR of naftopidil-based arylpiperazine derivatives

[Display omitted] For the development of potential anti-prostate cancer agents, 24 kinds of novel naftopidil-based arylpiperazine derivatives have been synthesized and characterized by spectroscopic methods. Their antitumor activities were evaluated against several classical prostate cancer cell lin...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2018-05, Vol.28 (9), p.1534-1539
Hauptverfasser:	Chen, Hong, Wang, Cai-Lu, Sun, Tao, Zhou, Zhan, Niu, Jiang-Xiu, Tian, Xiu-Mei, Yuan, Mu
Format:	Artikel
Sprache:	eng
Schlagworte:	Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology CCK-8 Cell Cycle Checkpoints - drug effects Cell Line, Tumor Cell Proliferation - drug effects Derivatives Dose-Response Relationship, Drug Drug Screening Assays, Antitumor Humans Molecular Structure Naphthalenes - chemistry Naphthalenes - pharmacology Piperazine - chemical synthesis Piperazine - chemistry Piperazine - pharmacology Piperazines - chemistry Piperazines - pharmacology Prostate cancer Structure-Activity Relationship Synthesis
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Zusammenfassung:	[Display omitted] For the development of potential anti-prostate cancer agents, 24 kinds of novel naftopidil-based arylpiperazine derivatives have been synthesized and characterized by spectroscopic methods. Their antitumor activities were evaluated against several classical prostate cancer cell lines including PC-3, LNCaP, and DU145. Among all the compounds, 9, 13, 17, 21 and 27 showed strong cytotoxic activities against DU145 cells (IC50
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2018.03.070