Beutler J A, Hamel E, Vlietinck A J, Haemers A, Rajan P, Roitman J N, Cardellina J H, Boyd M R
Laboratory of Drug Discovery Research and Development, Developmental Therapeutics Program, Division of Cancer Treatment and Diagnosis, National Cancer Institute, Frederick, Maryland 21702-1201, USA.
J Med Chem. 1998 Jun 18;41(13):2333-8. doi: 10.1021/jm970842h.
A series of 79 flavones related to centaureidin (3,6,4'-trimethoxy-5, 7,3'-trihydroxyflavone, 1) was screened for cytotoxicity in the NCI in vitro 60-cell line human tumor screen. The resulting cytotoxicity profiles of these flavones were compared for degree of similarity to the profile of 1. Selected compounds were further evaluated with in vitro assays of tubulin polymerization and [3H]colchicine binding to tubulin. Maximum potencies for tubulin interaction and production of differential cytotoxicity profiles characteristic of 1 were observed only with compounds containing hydroxyl substituents at C-3' and C-5 and methoxyl groups at C-3 and C-4'.
在国立癌症研究所（NCI）的体外60细胞系人肿瘤筛选中，对一系列与矢车菊素（3,6,4'-三甲氧基-5,7,3'-三羟基黄酮，1）相关的79种黄酮进行了细胞毒性筛选。比较了这些黄酮产生的细胞毒性谱与1的谱的相似程度。所选化合物通过微管蛋白聚合的体外测定和[3H]秋水仙碱与微管蛋白的结合进行进一步评估。仅在C-3'和C-5位含有羟基取代基且C-3和C-4位含有甲氧基的化合物中，观察到了微管蛋白相互作用的最大效力以及产生了1所特有的差异细胞毒性谱。
