期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 59, 期 12, 页码 5706-5720出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.6b00129
关键词
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资金
- Italian Association for Cancer Research (AIRC) [IG-14150, IG-16730, IG-15886]
- Italian Institute of Technology (IIT)
- University of Naples Federico II [14-CSP3-C03-141]
G-Quadruplex-binding compounds are currently perceived as possible anticancer therapeutics. Here, starting from a promising lead, a small series of novel hydrazone-based compounds were synthesized and evaluated as G-quadruplex binders. The in vitro G-quadruplex-binding properties of the synthesized compounds were investigated employing both human telomeric and oncogene promoter G-quadruplexes with different folding topologies as targets. The present investigation led to the identification of potent G-quadruplex stabilizers with high selectivity over duplex DNA and preference for one G-quadruplex topology over others. Among them, selected derivatives have been shown to trap G-quadruplex structures in the nucleus of cancer cells. Interestingly, this behavior correlates with efficient cytotoxic activity in human osteosarcoma and colon carcinoma cells.
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