Journal
BIOORGANIC CHEMISTRY
Volume 60, Issue -, Pages 30-36Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2015.04.002
Keywords
Acridone derivatives; Synthesis; Antiproliferative activity; G-quadruplex DNA
Funding
- Ministry of Science and Technology of China [2012AA020305, 2013AA092902]
- Chinese National Natural Science Foundation [21272134, 21372141]
- Shenzhen Sci Tech Bureau [ZDSY20120619141412872, JCYJ20120831165730905]
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A novel series of l0-(3,5-dimethoxy)benzyl-9(10H)-acridone derivatives with terminal ammonium substituents at C2 and C7 positions on the acridone ring were successfully synthesized as antiproliferation agents. The biologic activity of the acridone compounds against leukemia CCRF-CEM cells demonstrated that some of the compounds displayed good antiproliferative activity, among which compound 6a containing dimethylamine substituents at the terminal C2 and C7 positions exhibited the highest cytotoxicity with IC50 at 0.3 mu M. In addition compound 6a showed little toxicity against normal 293T cells proliferation with IC50 more than 100 mu M. Further study indicated that compound 6a had strong binding activity to human telomeric G-quadruplex DNA, as detected by mass spectrometry, CD spectroscopy, UV absorption, FRET and fluorescence quenching assays. Our data suggested that the activity of 6a might be associated with its stabilization of G-quadruplex DNA, which can be developed as potent antitumor agent. (C) 2015 Elsevier Inc. All rights reserved.
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