Evidence map›Paper›PMID 25027938›Full record

ArticleBioorganic & medicinal chemistry letters2014

Synthesis and receptor binding in trans-CD ring-fused A-CD estrogens: comparison with the cis-fused isomers.

Cristian Dabrota, Muhammad Asim, Christine Choueiri, Ana Gargaun, Ilia Korobkov, Ammara Butt, Kathryn E Carlson, John A Katzenellenbogen, James S Wright, Tony Durst

Open access · greenAbstract readComparative Study
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2014. 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
0.2field-weighted citation impact, top 35% 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

1 citing paper in PubMed, 2 citations in OpenAlex.

  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

10 authors at 3 institutions in 2 countries.

Cristian DabrotaDepartment of Chemistry, University of Ottawa, D'Iorio Hall, 10 Marie Curie St., Ottawa K1N 6N5, Canada.
Muhammad AsimDepartment of Chemistry, University of Ottawa, D'Iorio Hall, 10 Marie Curie St., Ottawa K1N 6N5, Canada.
Christine ChoueiriDepartment of Chemistry, University of Ottawa, D'Iorio Hall, 10 Marie Curie St., Ottawa K1N 6N5, Canada.
Ana GargaunDepartment of Chemistry, University of Ottawa, D'Iorio Hall, 10 Marie Curie St., Ottawa K1N 6N5, Canada.
Ilia KorobkovDepartment of Chemistry, University of Ottawa, D'Iorio Hall, 10 Marie Curie St., Ottawa K1N 6N5, Canada.
Ammara ButtDepartment of Chemistry, University of Ottawa, D'Iorio Hall, 10 Marie Curie St., Ottawa K1N 6N5, Canada.
Kathryn E CarlsonDepartment of Chemistry, University of Illinois, Urbana, IL 61801, USA.
John A KatzenellenbogenDepartment of Chemistry, University of Illinois, Urbana, IL 61801, USA.
James S WrightDepartment of Chemistry, Carleton University, 1125 Colonel By Dr., Ottawa K1S 5B6, Canada.
Tony DurstDepartment of Chemistry, University of Ottawa, D'Iorio Hall, 10 Marie Curie St., Ottawa K1N 6N5, Canada. Electronic address: tony.durst@uottawa.ca.
University of Ottawa · CAUniversity of Illinois Urbana-Champaign · USCarleton University · CA

Funding

Novel Ligands and Mechanisms to Achieve Selective Nuclear Receptor ActivityR01DK015556 · NIDDK · UNIVERSITY OF ILLINOIS URBANA-CHAMPAIGN · PI KATZENELLENBOGEN, JOHN A. · 1986 to 2016
$1.6M
NIDDK NIH HHS 5R01 DK015556NIDDK NIH HHS R01 DK015556
6 · The paper itself

Abstract

Ligands which selectively activate only one of the estrogen receptors, ERα or ERβ, are current pharmaceutical targets. Previously, we have reported on substituted cis A-CD ligands in which the B-ring of the steroidal structure has been removed and cis refers the stereochemistry of the CD ring junction as compared to trans in estradiol. These compounds often showed good potency and selectivity for ERβ. Here we report the synthesis and binding affinities for a similar series of trans A-CD ligands, and compare them to the cis-series. Counterintuitively, trans A-CD ligands, which are structurally more closely related to the natural ligand estradiol, show weaker binding and less β-selectivity than their cis-counterparts.

Indexed as

Crystallography, X-RayDose-Response Relationship, DrugEstrogen Receptor alphaEstrogen Receptor AntagonistsEstrogen Receptor betaHumansLigandsModels, MolecularMolecular ConformationStereoisomerismStructure-Activity RelationshipEstrogen Receptor alphaEstrogen Receptor AntagonistsEstrogen Receptor betaLigandsERαERβEstrogen receptorLigand synthesisβ-Selectivity

Identifiers

PMID25027938
PMCPMC4249688
OpenAlexW2027736455

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.