AIMing towards improved antitumor efficacy Dedicated to the memory of Professor Albert I. Meyers

Matthew J. Weaver, Alison K. Kearns, Sascha Stump, Chun Li, Mariusz P. Gajewski, Kevin C. Rider, Donald S. Backos, Philip R. Reigan, Howard D. Beall, Nicholas R. Natale

Research output: Contribution to journalArticlepeer-review

Abstract

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.

Original languageEnglish
Pages (from-to)1765-1770
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume25
Issue number8
DOIs
StatePublished - Apr 15 2015

Keywords

  • Anthracene
  • DNA Quadruplex
  • Glioblastoma
  • Isoxazole
  • Pyrrole
  • Tumor paint

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