Antitumor Activity and Structure-Activity Relationship of Diterpenoids with a Dehydroabietyl Skeleton

作者：Rao, Xiaoping^*; Huang, Xiuzhi; He, Ling; Song, Jie; Song, Zhanqian; Shang, Shibin

来源：Combinatorial Chemistry & High Throughput Screening, 2012, 15(10): 840-844.

DOI：10.2174/138620712803901199

• Antitumor activity
• dehydroabietyl skeleton
• diterpenoid
• structure-activity relationship

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.

• 出版日期2012-12
• 单位中国林业科学研究院; 中国药科大学