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Combinatorial Chemistry & High Throughput Screening


ISSN (Print): 1386-2073
ISSN (Online): 1875-5402

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

Author(s): Xiaoping Rao, Xiuzhi Huang, Ling He, Jie Song, Zhanqian Song and Shibin Shang

Volume 15, Issue 10, 2012

Page: [840 - 844] Pages: 5

DOI: 10.2174/138620712803901199

Price: $65


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.

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