Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 25, Issue 8, Pages 1765-1770Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2015.02.063
Keywords
Isoxazole; Anthracene; Pyrrole; DNA Quadruplex; Glioblastoma; Tumor paint
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Funding
- Nationals Institutes of Health [NINDS 7R15-NS038444-04, P20 RR015583, P20RR017670, P30 NS 055022, NIH/NCATS UL1 TR001082]
- ALSAM Foundation Skaggs Scholars Program
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Using the structure-activity relationship emerging from previous Letter, and guided by pharmacokinetic properties, new AIMs have been prepared with both improved efficacy against human glioblastoma cells and cell permeability as determined by fluorescent confocal microscopy. We present our first unambiguous evidence for telomeric G4-forming oligonucleotide anisotropy by NMR resulting from direct interaction with AIMs, which is consistent with both our G4 melting studies by CD, and our working hypothesis. Finally, we show that AIMs induce apoptosis in SNB-19 cells. (C) 2015 Elsevier Ltd. All rights reserved.
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