Antitumor Activity and Structure-Activity Relationship of Diterpenoids with a Dehydroabietyl Skeleton
Antitumor Activity and Structure-Activity Relationship of Diterpenoids with a Dehydroabietyl Skeleton
复制标题
DOI：
10.2174/138620712803901199
复制
发表时间：
2012-12-01
影响因子：
1.8
通讯作者：
Shang, Shibin
中科院分区：
文献类型：
--
作者：
Rao, Xiaoping;Huang, Xiuzhi;Shang, Shibin
采用MTT法筛选了一系列具有脱氢松香基骨架的亚胺类、酰胺类和脲类二萜化合物对肝癌细胞（SMMC-7721）、肺癌细胞（A-549）、胶质瘤细胞（C-6）和乳腺癌细胞（MCF-7）的抑制作用。并对其抗肿瘤活性及构效关系进行了分析。标题化合物I-2、I-10、I-6和I-5对SMMC-7721、A-549、C-6和MCF-7肿瘤细胞具有显著的抗肿瘤活性，最低IC_（50）值分别为6.65、0.75、0.81和10.65 μ M。构效关系研究表明，三种脱氢松香基骨架的二萜类化合物对SMMC-7721细胞均表现出较高的活性。亚胺类衍生物对所选的四种肿瘤细胞具有广谱、高效的活性。
A series of novel diterpenoids including imines, amides and ureas with a dehydroabietyl skeleton were screened to hepatocellular carcinoma (SMMC-7721), lung cancer (A-549), glioma (C-6) and breast carcinoma (MCF-7) tumor cells by MTT method. Their antitumor activity and structure activity relationship were analyzed. Several of the title compounds such as I-2, I-10, I-6 and I-5, possess noticeable antitumor activity against SMMC-7721, A-549, C-6 and MCF-7 tumor cells, with lowest IC50 values of 6.65, 0.75, 0.81 and 10.65 mu M, respectively. Based on the structure-activity relationship investigation, the three kinds of diterpenoids with a dehydroabietyl skeleton show high activity to SMMC-7721 cells. Imines derivatives exhibit broad spectrum and highly efficient activities to the selected four kinds of tumor cells.