Synthesis and evaluation of cytotoxic activities of new guanidines derived from carbazoles

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• 作者：Anna Caruso ; Maria Stefania Sinicropi ; Jean-Charles Lancelot ; Hussein El-Kashef ; Carmela Saturnino ; Genevi猫ve Aubert ; C茅line Ball ; onne ; Aur茅lien Lesnard ; Thierry Cresteil ; Patrick Dallemagne ; Sylvain Rault
• 关键词：Carbazoles ; Guanidinocarbazoles ; Guanidines ; KB ; HL60 ; MCF7 ; HCT116 ; PC3 ; MRC5
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：15 January, 2014
• 年：2014
• 卷：24
• 期：2
• 页码：467-472
• 全文大小：1223 K

文摘

Several new alkylguanidines derived from carbazole have been synthesized in a simple one-pot reaction starting from 3-aminocarbazole derivatives. The aminocarbazoles were reacted with ethoxycarbonylisothiocyanate, to give thiourea intermediates, followed by the addition of an alkylamine and HgCl₂ to give ethoxycarbonylguanidine intermediates. The reaction mixture was then heated at 160 掳C to give the N-(1,4-dimethyl-9H-carbazol-3-yl)-N鈥?alkylguanidines.

The cytotoxic activity of all the synthesized guanidines was evaluated against different cell lines.