☆ 4.7 Article

Synthesis and anticancer potential of novel xanthone derivatives with 3,6-substituted chains

BIOORGANIC & MEDICINAL CHEMISTRY (2016)

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

类别

Biochemistry & Molecular Biology Chemistry, Medicinal Chemistry, Organic

资金

UF Health Cancer Center startup funds

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Reagent

摘要

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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