Evidence map›Paper›PMID 20359224›Full record

ArticleJournal of medicinal chemistry2010

Macrocyclic pyridyl polyoxazoles: selective RNA and DNA G-quadruplex ligands as antitumor agents.

Suzanne G Rzuczek, Daniel S Pilch, Angela Liu, Leroy Liu, Edmond J LaVoie, Joseph E Rice

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.

0numbers the graph read from it
0cells of the map it votes in
15citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

15 citing papers in PubMed.

  1. Article
  2. Article
  3. Article
  4. The Hairpin Form of r(GCell chemical biology · 2019
    Article
  5. Article
  6. Article
  7. Article
  8. Article
  9. Dinickel-Salphen Complexes as Binders of Human Telomeric Dimeric G-Quadruplexes.Chemistry (Weinheim an der Bergstrasse, Germany) · 2017
    Article
  10. Article
  11. Review
  12. Article
  13. Article
  14. Article
  15. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

6 authors.

Suzanne G RzuczekDepartment of Medicinal Chemistry, Ernest Mario School of Pharmacy, Rutgers-The State University of New Jersey, 160 Frelinghuysen Road, Piscataway, New Jersey 08854-8020, USA.
Daniel S Pilch
Angela Liu
Leroy Liu
Edmond J LaVoie
Joseph E Rice

Funding

YOGA LIFESTYLE INTERVENTION REDUCES BLOOD PRESSURE IN HIV-INFECTED ADULTSP41RR000954 · NCRR · WASHINGTON UNIVERSITY · PI GROSS, MICHAEL L · 1985 to 2011
$16.0M
Purchase of a 400 MHz Multi-Nuclear NMR SpectrometerS10RR023698 · NCRR · RUTGERS, THE STATE UNIV OF N.J. · PI RICE, JOSEPH E · 2008 to 2008
$351k
NCRR NIH HHS 1S10RR23698-1A1NCRR NIH HHS P41 RR000954NCRR NIH HHS P41RR0954NCRR NIH HHS S10 RR023698
6 · The paper itself

Abstract

The synthesis of a series of 24-membered pyridine-containing polyoxazole macrocycles is described. Seventeen new macrocycles were evaluated for cytotoxic activity against RPMI 8402, KB-3, and KB-3 cell lines that overexpress the efflux transporters MDR1 (KBV-1) and BCRP (KBH5.0). Macrocycles in which the pyridyl-polyoxazole moiety is linked by a 1,3-bis(aminomethyl)phenyl group with a 5-(2-aminoethyl)- (18) or a 5-(2-dimethylaminoethyl)- substituent (19) displayed the greatest cytotoxic potency. These compounds exhibit exquisite selectivity for stabilizing G-quadruplex DNA with no stabilization of duplex DNA or RNA. Compound 19 stabilizes quadruplex mRNA that encodes the cell-cycle checkpoint protein kinase Aurora A to a greater extent than the quadruplex DNA of a human telomeric sequence. These data may suggest a role for G-quadruplex ligands interacting with mRNA being associated with the biological activity of macrocyclic polyoxazoles. Compound 19 has significant in vivo anticancer activity against a human breast cancer xenograft (MDA-MB-435) in athymic nude mice.

Indexed as

AnimalsAntineoplastic AgentsATP-Binding Cassette TransportersATP Binding Cassette Transporter, Subfamily BATP Binding Cassette Transporter, Subfamily B, Member 1ATP Binding Cassette Transporter, Subfamily G, Member 2Breast NeoplasmsCarrier ProteinsCell Line, TumorDNADrug Screening Assays, AntitumorG-QuadruplexesHumansLigandsMacrocyclic CompoundsMiceABCB1 protein, humanABCG2 protein, humanAntineoplastic AgentsATP-Binding Cassette TransportersATP Binding Cassette Transporter, Subfamily BATP Binding Cassette Transporter, Subfamily B, Member 1ATP Binding Cassette Transporter, Subfamily G, Member 2Carrier ProteinsDNALigandsMacrocyclic CompoundsNeoplasm ProteinsOxazolesPyridinesRNA

Identifiers

PMID20359224
PMCPMC2865558

What OpenQuestion holds

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Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.