期刊
MOLECULES
卷 17, 期 6, 页码 7067-7082出版社
MDPI
DOI: 10.3390/molecules17067067
关键词
acridine; DNA-binding drugs; solid-phase synthesis; G-quadruplex; NMR
资金
- Spanish Ministry of Education [BFU2007-63287, CTQ2010-20541-C03-01]
- Generalitat de Catalunya [2009/SGR/208]
- VI National R&D&i Plan, Iniciativa Ingenio, Consolider Program, CIBER Actions
- Instituto de Salud Carlos III
- PRIN09 [2009Prot.2009J54YAP_005]
- FPI from Spanish Ministry of Science
Several acridine derivatives were synthesized and their anti-proliferative activity was determined. The most active molecules were derivatives of 5-methylacridine-4-carboxylic acid. The DNA binding properties of the synthesized acridines were analyzed by competitive dialysis and compared with the anti-proliferative activities. While inactive acridine derivatives showed high selectivity for G-quadruplex structures, the most active 5-methylacridine-4-carboxamide derivatives had high affinity for DNA but showed poor specificity. An NMR titration study was performed with the most active 5-methylacridine-4-carboxamide, confirming the high affinity of this compound for both duplex and quadruplex DNAs.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据