Evidence map›Paper›PMID 24657571›Full record

ArticleEuropean journal of medicinal chemistry2014

Synthesis and functional survey of new Tacrine analogs modified with nitroxides or their precursors.

Tamás Kálai, Robin Altman, Izumi Maezawa, Mária Balog, Christophe Morisseau, Jitka Petrlova, Bruce D Hammock, Lee-Way Jin, James R Trudell, John C Voss and 1 more

Open access · bronzeAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in European journal of medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
2.5field-weighted citation impact, top 10% of its field
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

3 citing papers in PubMed, 13 citations in OpenAlex.

  1. Review
  2. Article
  3. Review
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

11 authors at 4 institutions in 2 countries.

Tamás KálaiInstitute of Organic and Medicinal Chemistry, University of Pécs, H-7624 Pécs, Szigeti St. 12. Pécs, Hungary.
Robin AltmanDepartment of Biochemistry & Molecular Medicine, University of California Davis, Davis, CA 95616, USA.
Izumi MaezawaM.I.N.D. Institute and Department of Pathology and Laboratory Medicine, University of California Davis, Sacramento, CA95817, USA.
Mária BalogInstitute of Organic and Medicinal Chemistry, University of Pécs, H-7624 Pécs, Szigeti St. 12. Pécs, Hungary.
Christophe MorisseauDepartment of Entomology and UC Davis Comprehensive Cancer Center, University of California Davis, Davis, CA 95616, USA.
Jitka PetrlovaDepartment of Biochemistry & Molecular Medicine, University of California Davis, Davis, CA 95616, USA.
Bruce D HammockDepartment of Entomology and UC Davis Comprehensive Cancer Center, University of California Davis, Davis, CA 95616, USA.
Lee-Way JinM.I.N.D. Institute and Department of Pathology and Laboratory Medicine, University of California Davis, Sacramento, CA95817, USA.
James R TrudellDepartment of Anesthesia, Beckman Program for Molecular and Genetic Medicine, Stanford University, Stanford, CA 94305-5117, USA.
John C VossDepartment of Biochemistry & Molecular Medicine, University of California Davis, Davis, CA 95616, USA.
Kálmán HidegInstitute of Organic and Medicinal Chemistry, University of Pécs, H-7624 Pécs, Szigeti St. 12. Pécs, Hungary. Electronic address: kalman.hideg@aok.pte.hu.
University of California, Davis · USUniversity of Pecs · HUStanford University · USUC Davis Comprehensive Cancer Center

Funding

HYDROLYTIC ENZYMES IN THE METABOLISM OF TOXINSR01ES002710 · NIEHS · UNIVERSITY OF CALIFORNIA DAVIS · PI HAMMOCK, BRUCE D · 1985 to 2018
$4.0M
Defining Alcohol Binding Sites in Ligand-Gated Ion ChannelsR01AA020980 · NIAAA · STANFORD UNIVERSITY · PI BERTACCINI, EDWARD J · 2013 to 2017
$1.6M
The structural basis of apoE4's role in Alzheimer's DiseaseR01AG029246 · NIA · UNIVERSITY OF CALIFORNIA AT DAVIS · PI VOSS, JOHN CARL · 2007 to 2011
$1.3M
NIAAA NIH HHS R01 AA020980NIAAA NIH HHS R01AA02098001A1NIA NIH HHS R01 AG029246NIEHS NIH HHS R01 ES002710
6 · The paper itself

Abstract

A series of new Tacrine analogs modified with nitroxides or pre-nitroxides on 9-amino group via methylene or piperazine spacers were synthesized; the nitroxide or its precursors were incorporated into the Tacrine scaffold. The new compounds were tested for their hydroxyl radical and peroxyl radical scavenging ability, acetylcholinesterase inhibitor activity and protection against Aβ-induced cytotoxicity. Based on these assays, we conclude that Tacrine analogs connected to five and six-membered nitroxides via piperazine spacers (9b, 9b/HCl and 12) exhibited the best activity, providing direction for further development of additional candidates with dual functionality (anti Alzheimer's and antioxidant).

Indexed as

AcetylcholinesteraseAntineoplastic AgentsAntioxidantsCell Line, TumorCell ProliferationCholinesterase InhibitorsDose-Response Relationship, DrugDrug Screening Assays, AntitumorHumansModels, MolecularMolecular StructureNitrogen OxidesStructure-Activity RelationshipTacrineAcetylcholinesteraseAntineoplastic AgentsAntioxidantsCholinesterase InhibitorsNitrogen OxidesTacrineAlzheimer's diseaseAntioxidantsNitroxidesSpin trappingTacrine

Identifiers

PMID24657571
PMCPMC4065883
OpenAlexW2022060532

What OpenQuestion holds

Textmetadata
LicenceTDM
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.