Rao Xiaoping, Huang Xiuzhi, He Ling, Song Jie, Song Zhanqian, Shang Shibin
Institute of Chemical Industry of Forestry Products, CAF, Key Lab. of Biomass Energy and Material, Jiangsu Province, National Engineering Lab. for Biomass Chemical Utilization; Key and Lab. on Forest Chemical Engineering, SFA, Nanjing 210042, China.
Comb Chem High Throughput Screen. 2012 Dec;15(10):840-4. doi: 10.2174/138620712803901199.
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 IC(50) values of 6.65, 0.75, 0.81 and 10.65μM, 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.
通过MTT法对一系列具有脱氢枞基骨架的新型二萜类化合物（包括亚胺、酰胺和脲）进行了筛选，以检测其对肝癌（SMMC-7721）、肺癌（A-549）、胶质瘤（C-6）和乳腺癌（MCF-7）肿瘤细胞的活性。分析了它们的抗肿瘤活性及构效关系。几种目标化合物，如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10.65μM。基于构效关系研究，三种具有脱氢枞基骨架的二萜类化合物对SMMC-7721细胞表现出高活性。亚胺衍生物对所选的四种肿瘤细胞表现出广谱高效的活性。
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