期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 18, 页码 5496-5499出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.07.090
关键词
Gibberellins; alpha,beta-Unsaturated ketone; Cytotoxic activities; Diterpenes
资金
- Yunnan Provincial Science & Technology Department [2007B0006Z]
- Chinese Ministry of Education [706052]
- National Natural Science Foudation of China [30660213, 20562013]
A series of gibberellin based molecules were designed and synthesized. Gibberellin derivatives bearing two alpha,beta-unsaturated ketone units showed strong anticancer activities in MTT assay towards a number of human cancer cell lines including HT29, A549, HepG2 and MKN28. The most potent gibberellin derivative (compound 10, IC50 = 2.9 mu M against HT29) inhibited completely the topoisomerase I activity at 8 mu g/ml. level. (C) 2009 Elsevier Ltd. All rights reserved.
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