title: AIMing towards improved antitumor efficacy.
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.
authors.affiliation: Department of Biomedical and Pharmaceutical Sciences, University of Montana, Missoula, MT 59812, United States.
authors.forename: Matthew J
authors.initials: MJ
authors.lastname: Weaver
authors.affiliation: Department of Biomedical and Pharmaceutical Sciences, University of Montana, Missoula, MT 59812, United States.
authors.forename: Alison K
authors.initials: AK
authors.lastname: Kearns
authors.affiliation: Department of Biomedical and Pharmaceutical Sciences, University of Montana, Missoula, MT 59812, United States.
authors.forename: Sascha
authors.initials: S
authors.lastname: Stump
authors.affiliation: Department of Chemistry, Ithaca College, 953 Danby Road, Ithaca, NY 14850, United States.
authors.forename: Chun
authors.initials: C
authors.lastname: Li
authors.affiliation: Department of Chemistry, Arkansas Tech University, Russellville, AR 72801, United States.
authors.forename: Mariusz P
authors.initials: MP
authors.lastname: Gajewski
authors.affiliation: Department of Biomedical and Pharmaceutical Sciences, University of Montana, Missoula, MT 59812, United States.
authors.forename: Kevin C
authors.initials: KC
authors.lastname: Rider
authors.affiliation: Skaggs School of Pharmacy and Pharmaceutical Sciences, Anschutz Medical Campus, University of Colorado Denver, Aurora, CO 80045, United States.
authors.forename: Donald S
authors.initials: DS
authors.lastname: Backos
authors.affiliation: Skaggs School of Pharmacy and Pharmaceutical Sciences, Anschutz Medical Campus, University of Colorado Denver, Aurora, CO 80045, United States. Electronic address: philip.reigan@ucdenver.edu.
authors.forename: Philip R
authors.initials: PR
authors.lastname: Reigan
authors.affiliation: Department of Biomedical and Pharmaceutical Sciences, University of Montana, Missoula, MT 59812, United States. Electronic address: howard.beall@umontana.edu.
authors.forename: Howard D
authors.initials: HD
authors.lastname: Beall
authors.affiliation: Department of Biomedical and Pharmaceutical Sciences, University of Montana, Missoula, MT 59812, United States. Electronic address: nicholas.natale@umontana.edu.
authors.forename: Nicholas R
authors.initials: NR
authors.lastname: Natale
mesh_terms: D000577:Amides / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D017209:Apoptosis; D001665:Binding Sites; D045744:Cell Line, Tumor; D002942:Circular Dichroism; D018360:Crystallography, X-Ray; D054856:G-Quadruplexes; D006801:Humans; D056004:Molecular Dynamics Simulation; D009690:Nucleic Acid Conformation; D013329:Structure-Activity Relationship; D016615:Telomere / Q000737:chemistry
chemical_list: D000577:Amides; D000970:Antineoplastic Agents
keywords: Anthracene; DNA Quadruplex; Glioblastoma; Isoxazole; Pyrrole; Tumor paint