期刊
BIOORGANIC CHEMISTRY
卷 68, 期 -, 页码 137-151出版社
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2016.08.004
关键词
Oleanolic acid; Amides; Tumor cells; Cell-cycle arrest; Apoptosis; Autophagy
资金
- WissenschaftsCampus Halle WCH
- Oman Research Council [ORG/HSS/14/004]
Thirty-one different 3-O-acetyl-OA derived amides have been prepared and screened for their cytotoxic activity. In the SRB assays nearly all the carboxamides displayed good cytotoxicity in the low mu M range for several human tumor cell lines. Low EC50 values were obtained especially for the picolinylamides 14-16, for a N-[2-(dimethylamino)-ethyl] derivative 27 and a N-[2-(pyrrolinyl)-ethyl] carboxamide 28. These compounds were submitted to an extensive biological testing and proved compound 15 to act mainly by an arrest of the tumor cells in the S phase of the cell cycle. Cell death occurred by autophagy while compounds 27 and 28 triggered apoptosis. (C) 2016 Elsevier Inc. All rights reserved.
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