期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 3, 页码 1004-1009出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.12.019
关键词
Pharmacophore modeling; Virtual screening; Telomeric G-quadruplex DNA; Acridine derivatives; Triaryl-substituted imidazole
资金
- Natural Science Foundation of China [U0832005, 90813011, 20772159, 81001400]
- Science Foundation of Guangzhou [2009A1-E011-6]
Discovery of potent and selective ligands for telomeric G-quadruplex DNA is a challenging work. Through a combination approach of pharmacophore model construction, model validation, database virtual screening, chemical synthesis and interaction evaluation, we discovered and confirmed triaryl-substituted imidazole TSIZ01 to be a new telomeric G-quadruplex ligand with potent binding and stabilizing activity to G-quadruplex DNA, as well as a 8.7-fold selectivity towards telomeric G-quadruplex DNA over duplex DNA. (C) 2010 Elsevier Ltd. All rights reserved.
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