Evidence map›Paper›PMID 31370197›Full record

ArticleMolecules (Basel, Switzerland)2019

A Structure-Activity Relationship Study of Bis-Benzamides as Inhibitors of Androgen Receptor-Coactivator Interaction.

Tae-Kyung Lee, Preethi Ravindranathan, Rajni Sonavane, Ganesh V Raj, Jung-Mo Ahn

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Molecules (Basel, Switzerland), 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing 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

2 citing papers in PubMed.

  1. Review
  2. Aromatic oligoesters as novel helix mimetic scaffolds.Bioorganic & medicinal chemistry · 2023
    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

5 authors.

Tae-Kyung LeeDepartment of Chemistry and Biochemistry, University of Texas at Dallas, Richardson, TX 75080, USA.
Preethi RavindranathanDepartments of Urology and Pharmacology, University of Texas Southwestern Medical Center at Dallas, Dallas, TX 75390, USA.
Rajni SonavaneDepartments of Urology and Pharmacology, University of Texas Southwestern Medical Center at Dallas, Dallas, TX 75390, USA.
Ganesh V RajDepartments of Urology and Pharmacology, University of Texas Southwestern Medical Center at Dallas, Dallas, TX 75390, USA.
Jung-Mo AhnDepartment of Chemistry and Biochemistry, University of Texas at Dallas, Richardson, TX 75080, USA. jungmo.ahn@utdallas.edu.ORCID 0000-0002-9104-525X

Funding

Cancer Prevention and Research Institute of Texas RP120717-P4U.S. Department of Defense W81XWH-12-1-0288Welch Foundation AT-1595
6 · The paper itself

Abstract

The interaction between androgen receptor (AR) and coactivator proteins plays a critical role in AR-mediated prostate cancer (PCa) cell growth, thus its inhibition is emerging as a promising strategy for PCa treatment. To develop potent inhibitors of the AR-coactivator interaction, we have designed and synthesized a series of bis-benzamides by modifying functional groups at the N/C-terminus and side chains. A structure-activity relationship study showed that the nitro group at the N-terminus of the bis-benzamide is essential for its biological activity while the C-terminus can have either a methyl ester or a primary carboxamide. Surveying the side chains with various alkyl groups led to the identification of a potent compound

Indexed as

Androgen AntagonistsBenzamidesCell Line, TumorCell ProliferationCo-Repressor ProteinsGene Expression Regulation, NeoplasticHumansMaleProstate-Specific AntigenProstatic NeoplasmsProtein Conformation, alpha-HelicalProtein Interaction MapsReceptors, AndrogenStructure-Activity RelationshipTranscriptional ActivationTranscription FactorsAndrogen AntagonistsAR protein, humanBenzamidesCo-Repressor ProteinsPELP1 protein, humanProstate-Specific AntigenReceptors, AndrogenTranscription Factorsandrogen receptorbis-benzamide scaffoldcoactivator PELP1prostate cancerprotein–protein interactionα-helix mimetics

Identifiers

PMID31370197
PMCPMC6696232

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Registered trials

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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.