Synthesis and Biological Evaluation of 2-(3',4',5'-Trimethoxybenzoyl)-3-Amino 5-Aryl Thiophenes as a New Class of Tubulin Inhibitors

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• 作者：Romeo Romagnoli ; Pier Giovanni Baraldi ; Vincent Remusat ; Maria Dora Carrion ; Carlota Lopez Cara ; Delia Preti ; Francesca Fruttarolo ; Maria Giovanna Pavani ; Mojgan Aghazadeh Tabrizi ; Manlio Tolomeo ; Ste
• 刊名：Journal of Medicinal Chemistry
• 出版年：2006
• 出版时间：October 19, 2006
• 年：2006
• 卷：49
• 期：21
• 页码：6425 - 6428
• 全文大小：72K
• 年卷期：v.49,no.21(October 19, 2006)
• ISSN：1520-4804

文摘

2-(3',4',5'-Trimethoxybenzoyl)-3-amino-5-aryl/heteroaryl thiophene derivatives were synthesized and evaluatedfor antiproliferative activity, inhibition of tubulin polymerization, and cell cycle effects. SARs were elucidatedwith various substitutions on the aryl moiety 5-position of the thienyl ring. Substituents at the para-positionof the 5-phenyl group showed antiproliferative activity in the order of F=CH₃ > OCH₃=Br=NO₂ > CF₃=I > OEt. Several of these compounds led to arrest of HL-60 cells in the G2/M phase of the cell cycle andinduction of apoptosis.