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

doi:10.1016/j.bmcl.2015.02.063

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 journal › Article › peer-review

8 Scopus citations

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 language	English
Pages (from-to)	1765-1770
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	25
Issue number	8
DOIs	https://doi.org/10.1016/j.bmcl.2015.02.063
State	Published - Apr 15 2015

Funding

We thank the Nationals Institutes of Health for grants NINDS 7R15-NS038444-04 (N.R.N.), P20 RR015583 (N.R.N., M.P.G.), P20RR017670 (H.D.B.), P30 NS 055022 (K.C.R., N.R.N.), NIH/NCATS UL1 TR001082 (D.S.B., P.R.R.) and the ALSAM Foundation Skaggs Scholars Program (P.R.R., H.D.B., N.R.N.). We thank Dr, Earle Adams for his assistance with oligonucleotide NMR, Pam Shaw for help with the fluorescence studies, and Professor Bruce Bowler’s laboratory for advice and use of his CD.

Funder number
7R15-NS038444-04, P30NS055022, P20 RR015583
P20RR017670
UL1 TR001082

Keywords

Anthracene
DNA Quadruplex
Glioblastoma
Isoxazole
Pyrrole
Tumor paint

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10.1016/j.bmcl.2015.02.063

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title = "AIMing towards improved antitumor efficacy Dedicated to the memory of Professor Albert I. Meyers",

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.",

keywords = "Anthracene, DNA Quadruplex, Glioblastoma, Isoxazole, Pyrrole, Tumor paint",

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

year = "2015",

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doi = "10.1016/j.bmcl.2015.02.063",

language = "English",

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journal = "Bioorganic and Medicinal Chemistry Letters",

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T1 - AIMing towards improved antitumor efficacy Dedicated to the memory of Professor Albert I. Meyers

AU - Weaver, Matthew J.

AU - Kearns, Alison K.

AU - Stump, Sascha

AU - Li, Chun

AU - Gajewski, Mariusz P.

AU - Rider, Kevin C.

AU - Backos, Donald S.

AU - Reigan, Philip R.

AU - Beall, Howard D.

AU - Natale, Nicholas R.

PY - 2015/4/15

Y1 - 2015/4/15

N2 - 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.

AB - 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.

KW - Anthracene

KW - DNA Quadruplex

KW - Glioblastoma

KW - Isoxazole

KW - Pyrrole

KW - Tumor paint

UR - https://www.scopus.com/pages/publications/84940008145

U2 - 10.1016/j.bmcl.2015.02.063

DO - 10.1016/j.bmcl.2015.02.063

M3 - Article

C2 - 25782743

AN - SCOPUS:84940008145

SN - 0960-894X

VL - 25

SP - 1765

EP - 1770

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 8

ER -

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

Abstract

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Keywords

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