Tubulin Binding, Protein-Bound Conformation in Solution, and Antimitotic Cellular Profiling of Noscapine and Its Derivatives

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• 作者：Youssef L. Bennani ; Wenxin Gu ; Angeles Canales ; Fernando J. Dı ; ́ ; az ; Brenda K. Eustace ; Russell R. Hoover ; Jesus Jim茅nez-Barbero ; Azin Nezami ; Tiansheng Wang
• 刊名：Journal of Medicinal Chemistry
• 出版年：2012
• 出版时间：March 8, 2012
• 年：2012
• 卷：55
• 期：5
• 页码：1920-1925
• 全文大小：262K
• 年卷期：v.55,no.5(March 8, 2012)
• ISSN：1520-4804

文摘

Noscapine and its 7-hydroxy and 7-amino derivatives were characterized for their binding to tubulin. A solution NMR structure of these compounds bound to tubulin shows that noscapine and its 7-aniline derivative do not compete for the same binding site nor does its small molecule crystal structure match its tubulin-bound conformation. These compounds were also tested for their antiproliferative effects on a panel hepatocellular carcinoma cell lines.