Vertex Pharmaceuticals Inc., 130 Waverly Street, Cambridge Massachusetts 02139, USA.
J Med Chem. 2012 Mar 8;55(5):1920-5. doi: 10.1021/jm200848t. Epub 2012 Feb 27.
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.
纳库巴因及其 7-羟基和 7-氨基衍生物的结合特性进行了研究。这些化合物与微管蛋白结合的溶液 NMR 结构表明,纳库巴因及其 7-苯胺衍生物不竞争相同的结合位点,其小分子晶体结构也与其微管蛋白结合构象不匹配。这些化合物还在一组肝癌细胞系中进行了抗增殖作用测试。