期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 24, 期 18, 页码 4263-4271出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2016.07.020
关键词
Xanthone derivatives; 3,6-Substituted long chains; Synthesis; Anticancer potential; IC50; A549; Structure-activity relationship; Apoptosis; Cell cycle arrest; Caspase 3/7 activity
资金
- UF Health Cancer Center startup funds
In an effort to develop new drug candidates with enhanced anticancer activity, our team synthesized and assessed the cytotoxicity of a series of novel xanthone derivatives with two longer 3,6-disubstituted amine carbonyl methoxy side chains on either benzene ring in selected human cancer cell lines. An MTT assay revealed that a set of compounds with lower IC50 values than the positive control, 5-FU, exhibited greater anticancer effects. The most potent derivative (XD8) exhibited anticancer activity in MDA-MB-231, PC-3, A549, AsPC-1, and HCT116 cells lines with IC50 values of 8.06, 6.18, 4.59, 4.76, and 6.09 mu M, respectively. Cell cycle analysis and apoptosis activation suggested that the mechanism of action of these derivatives includes cell cycle regulation and apoptosis induction. (C) 2016 Elsevier Ltd. All rights reserved.
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