Synthesis and evaluation of 10-(3,5-dimethoxy)benzyl-9(10H)-acridone derivatives as selective telomeric G-quadruplex DNA ligands |
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| Authors: | Chunmei Gao Shangfu Li Xuliang Lang Hongxia Liu Feng Liu Chunyan Tan Yuyang Jiang |
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| Affiliation: | 1. The Ministry-Province Jointly Constructed Base for State Key Lab-Shenzhen Key Laboratory of Chemical Biology, The Graduate School at Shenzhen, Tsinghua University, Shenzhen 518-55, PR China;2. Shenzhen Anti-Tumor Drug Development Engineering Laboratory, the Graduate School at Shenzhen, Tsinghua University, Shenzhen 518055, PR China;3. The Key Laboratory of Tumor Metabolomics at Shenzhen City, Shenzhen 518055, PR China;4. Department of Chemistry, Tsinghua University, Beijing 100084, PR China;5. Department of Pharmacology and Pharmaceutical Sciences, School of Medicine, Tsinghua University, Beijing 100084, PR China |
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| Abstract: | A class of 9(10H)-acridone derivatives with terminal ammonium substituents at C2 (and C7) position(s) on the acridone ring were successfully synthesized. The relative affinities of the acridone compounds to G-quadruplex DNA have been investigated and the results showed that these compounds had a binding specificity for G-quadruplex over duplex sequences. The acridones with two terminal ammonium substituents had much more effects on the human telomeric G-quadruplex DNA than the corresponding acridone derivatives with one terminal ammonium substituent, and more positive charges introduced to the side chains can improve the formation and stabilization of the G-quadruplex. |
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