Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 23, Issue 24, Pages 6755-6758Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.10.028
Keywords
Maleopimaric acid; Diimides; Atropisomers; Cytotoxicity; Apoptosis
Categories
Funding
- 973 project [2011CB512005]
- National Natural Science Foundation of China [81260472, 21101035]
- Guangxi Natural Science Foundation of China [2011GXNSFD018010, 12118008-10]
- Bagui Scholar project
- Foundation of Ministry of Education Innovation Team [IRT1225]
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Maleopimaric acid N-aryl imides (2) and methyl maleopimaric acid N-aryl imides (3) were designed and synthesized. Their atropisomers (A and B) were separated into their enantiomeric pure forms and the anti-proliferative activity was tested against NCI, A549, Hep G-2, MGC-803 and Hct-116 cell lines, respectively. A significant difference in the level of cytotoxicity was observed between R and S conformers. Atropisomers A with an R configuration exhibited significant toxicity (the IC50 values ranging from 7.51 to 32.1 mu M). Further experiments proved that antitumor activity of 2A was achieved through the induction of cell apoptosis by G1 cell-cycle arrest. (C) 2013 Elsevier Ltd. All rights reserved.
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