期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 16, 期 18, 页码 8670-8675出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2008.07.086
关键词
acridinone derivatives; antileukemia agent; antiproliferative activity; apoptosis
资金
- Ministry of Science and Technology of China [2007AA02Z160]
- Chinese National Natural Science Foundation [20672068, 20472043]
- China Postdoctoral Science Foundation [20070410547]
A novel series of 10-benzyl-9(10H)-acridinones and 1-benzyl-4-piperidones were synthesized and tested for their in vitro antitumor activities against CCRF-CEM cells. Assay-based antiproliferative activity study using CCRF-CEM cell lines revealed that the acridone group and the substitution pattern on the benzene unit had significant effect on cytotoxicity of this series of compounds, among which 10-(3,5-dimethoxy) benzyl-9(10H)-acridinone (3b) was found to be the most active compound with IC(50) at about 0.7 mu M. Compound 3b was also found to have antiproliferative activity against two other human leukemic cell lines K562 and HL60 using the MTT assay. The antitumor effect of 3b is believed to be due to the induction of apoptosis, which is further confirmed by PI ( Propidium iodide) staining and Annexin V-FITC/PI staining assay using flow cytometry analysis. (C) 2008 Elsevier Ltd. All rights reserved.
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