Evidence map›Paper›PMID 18776543›Full record

ArticleNucleic acids symposium series (2004)2008

Design and synthesis of truncated 4'-thioadenosine derivatives as potent and selective A3 adenosine receptor antagonists.

Xiyan Hou, Shantanu Pal, Won Jun Choi, Hea Ok Kim, Amol Tipnis, Kenneth A Jacobson, Lak Shin Jeong

Abstract read
In one paragraph

Article in Nucleic acids symposium series (2004), 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing 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

1 citing paper in PubMed.

  1. 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

7 authors.

Xiyan HouLaboratory of Medicinal Chemistry, College of Pharmacy, Ewha Womans University, Seoul 120-750, Korea.
Shantanu Pal
Won Jun Choi
Hea Ok Kim
Amol Tipnis
Kenneth A Jacobson
Lak Shin Jeong

Funding

Development Of Drugs Acting At Adenosine ReceptorsZIADK031117 · NIDDK · NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES · PI JACOBSON, KENNETH ALAN · 2009 to 2025
$10.4M
Drugs that Act at Adenosine ReceptorsZ01DK031117 · NIDDK · NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES · PI JACOBSON, KENNETH ALAN · 1991 to 2008
$854k
Intramural NIH HHS Z01 DK031117Intramural NIH HHS Z99 DK999999
6 · The paper itself

Abstract

We have established structure-activity relationships of novel truncated D-4'-thioadenosine derivatives from D-mannose as potent and selective A(3) adenosine receptor (AR) antagonists. At the human A(3) AR, most of N(6)-substituted analogues showed high potency and selectivity and acted as pure antagonists in a cyclic AMP functional assay. Among compounds tested, 2-chloro-N(6)-3-chlorobenzyl and N(6)-3-chlorobenzyl analogues displayed very high binding affinities (K(i) = 1.66 nM and 1.5 nM, respectively) at the human A(3) AR. Truncated 4'-thioadenosine derivatives studied here are regarded as an excellent template for the design of novel A(3) AR antagonists to act at both human and murine species.

Indexed as

Adenosine A3 Receptor AntagonistsAdenosineAnimalsCell LineCricetinaeDrug DesignHumansReceptor, Adenosine A3Structure-Activity RelationshipThionucleosides4'-thioadenosineAdenosineAdenosine A3 Receptor AntagonistsReceptor, Adenosine A3Thionucleosides

Identifiers

PMID18776543
PMCPMC3097420

What OpenQuestion holds

Textmetadata
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.