Evidence map›Paper›PMID 27179215›Full record

ArticleEuropean journal of medicinal chemistry2016

Symmetrical bis-tertiary amines as novel CXCR4 inhibitors.

Renren Bai, Zhongxing Liang, Younghyoun Yoon, Shuangping Liu, Theresa Gaines, Yoonhyeun Oum, Qi Shi, Suazette Reid Mooring, Hyunsuk Shim

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in European journal of medicinal chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing papers in PubMed
2.0field-weighted citation impact, top 12% 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

6 citing papers in PubMed, 22 citations in OpenAlex.

  1. Article
  2. Development of CXCR4 modulators based on the lead compound RB-108.European journal of medicinal chemistry · 2019
    Article
  3. Article
  4. Article
  5. Article
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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

9 authors at 2 institutions in 1 country.

Renren BaiDepartment of Radiology and Imaging Science, Emory University School of Medicine, Atlanta, GA, 30322, USA.
Zhongxing LiangDepartment of Radiology and Imaging Science, Emory University School of Medicine, Atlanta, GA, 30322, USA; Winship Cancer Institute, Emory University, Atlanta, GA, 30322, USA.
Younghyoun YoonDepartment of Radiology and Imaging Science, Emory University School of Medicine, Atlanta, GA, 30322, USA.
Shuangping LiuDepartment of Hematology and Medical Oncology, Emory University School of Medicine, Atlanta, GA, 30322, USA.
Theresa GainesDepartment of Chemistry, Georgia State University, Atlanta, GA, 30303, USA.
Yoonhyeun OumDepartment of Radiology and Imaging Science, Emory University School of Medicine, Atlanta, GA, 30322, USA.
Qi ShiDepartment of Chemistry, Emory University, Atlanta, GA, 30322, USA.
Suazette Reid MooringDepartment of Chemistry, Georgia State University, Atlanta, GA, 30303, USA. Electronic address: smooring@gsu.edu.
Hyunsuk ShimDepartment of Radiology and Imaging Science, Emory University School of Medicine, Atlanta, GA, 30322, USA; Winship Cancer Institute, Emory University, Atlanta, GA, 30322, USA. Electronic address: hshim@emory.edu.
Emory University · USGeorgia State University · US

Funding

Development of anti-CXCR4 compounds to block breast cancer metastasisR01CA165306 · NCI · EMORY UNIVERSITY · PI SHIM, HYUNSUK · 2012 to 2016
$1.7M
Development of anti-CXCR4 compounds as anti-metastatic, angiogenic drugR01CA109366 · NCI · EMORY UNIVERSITY · PI SHIM, HYUNSUK · 2006 to 2010
$1.3M
NCI NIH HHS R01 CA109366NCI NIH HHS R01 CA165306
6 · The paper itself

Abstract

CXCR4 inhibitors are promising agents for the treatment of cancer metastasis and inflammation. A series of novel tertiary amine derivatives targeting CXCR4 were designed, synthesized, and evaluated. The central benzene ring linker and side chains were modified and optimized to study the structure-activity relationship. Seven compounds displayed much more potent activity than the reference drug, AMD3100, in both the binding affinity assay and the blocking of Matrigel invasion functional assay. These compounds exhibited effective concentration ranging from 1 to 100 nM in the binding affinity assay and inhibited invasion from 65.3% to 100% compared to AMD3100 at 100 nM. Compound IIn showed a 50% suppressive effect against carrageenan-induced paw inflammation in a mouse model, which was as effective as the peptidic antagonist, TN14003 (48%). These data demonstrate that symmetrical bis-tertiary amines are unique CXCR4 inhibitors with high potency.

Indexed as

Drug DesignAminesAnimalsAnti-Inflammatory Agents, Non-SteroidalEdemaMiceMolecular Docking SimulationProtein ConformationReceptors, CXCR4Structure-Activity RelationshipAminesAnti-Inflammatory Agents, Non-SteroidalReceptors, CXCR4Anti-inflammatory activityBinding affinityCXCR4 inhibitorsMatrigel invasionTertiary amines

Identifiers

PMID27179215
PMCPMC4894032
OpenAlexW2339681187

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.