期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 17, 页码 5109-5113出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.07.033
关键词
Quadruplex ligands; Acridones; DNA binding
资金
- CRUK
- EU FP6 [LSHCCT2004-502943]
A series of 4,5-di-substituted acridones have been designed and synthesized. Several compounds show high affinity for telomeric G-quadruplex DNA in classical and competition FRET assays, together with low duplex DNA affinity, although they do not show activity in a telomerase assay or evidence of telomere shortening. They have low toxicity against a panel of cancer cell lines and a normal human fibroblast line, and produce potent senescence-based long-term growth arrest in the MCF7 and A549 cancer cell lines. (C) 2009 Elsevier Ltd. All rights reserved.
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