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

[ Vol. 15 , Issue. 10 ]

Author(s):

Xiaoping Rao, Xiuzhi Huang, Ling He, Jie Song, Zhanqian Song and Shibin Shang   Pages 840 - 844 ( 5 )

Abstract:


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 10.65μM, 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.

Keywords:

Antitumor activity, dehydroabietyl skeleton, diterpenoid, structure-activity relationship.

Affiliation:

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



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