Evidence map›Paper›PMID 25462258›Full record

ArticleEuropean journal of medicinal chemistry2015

Design, synthesis and biological evaluation of biphenylamide derivatives as Hsp90 C-terminal inhibitors.

Huiping Zhao, Gaurav Garg, Jinbo Zhao, Elisabetta Moroni, Antwan Girgis, Lucas S Franco, Swapnil Singh, Giorgio Colombo, Brian S J Blagg

Open access · bronzeAbstract read
In one paragraph

Article in European journal of medicinal chemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.

0numbers the graph read from it
0cells of the map it votes in
13citing papers in PubMed
3.4field-weighted citation impact, top 7% 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

13 citing papers in PubMed, 42 citations in OpenAlex.

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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 2 countries.

Huiping ZhaoDepartment of Medicinal Chemistry, 1251 Wescoe Hall Drive, Malott 4070, The University of Kansas, Lawrence, KS 66045-7563, USA.
Gaurav GargDepartment of Medicinal Chemistry, 1251 Wescoe Hall Drive, Malott 4070, The University of Kansas, Lawrence, KS 66045-7563, USA.
Jinbo ZhaoDepartment of Medicinal Chemistry, 1251 Wescoe Hall Drive, Malott 4070, The University of Kansas, Lawrence, KS 66045-7563, USA.
Elisabetta MoroniIstituto di chimica del riconoscimento molecolare, CNR, Via Mario Bianco 9, 20131 Milano, Italy.
Antwan GirgisDepartment of Medicinal Chemistry, 1251 Wescoe Hall Drive, Malott 4070, The University of Kansas, Lawrence, KS 66045-7563, USA.
Lucas S FrancoDepartment of Medicinal Chemistry, 1251 Wescoe Hall Drive, Malott 4070, The University of Kansas, Lawrence, KS 66045-7563, USA.
Swapnil SinghDepartment of Medicinal Chemistry, 1251 Wescoe Hall Drive, Malott 4070, The University of Kansas, Lawrence, KS 66045-7563, USA.
Giorgio ColomboIstituto di chimica del riconoscimento molecolare, CNR, Via Mario Bianco 9, 20131 Milano, Italy.
Brian S J BlaggDepartment of Medicinal Chemistry, 1251 Wescoe Hall Drive, Malott 4070, The University of Kansas, Lawrence, KS 66045-7563, USA. Electronic address: bblagg@ku.edu.
University of Kansas · USInstitute of Chemistry of Molecular Recognition · IT

Funding

Development and Evaluation of Purine and Coumarin Based Hsp90 Inhibitors`U01CA120458 · NCI · UNIVERSITY OF KANSAS LAWRENCE · PI BLAGG, BRIAN S J · 2007 to 2014
$2.6M
Development and Evaluation of Purine and Coumarin Based Hsp90 Inhibitors`R01CA120458 · NCI · UNIVERSITY OF NOTRE DAME · PI BLAGG, BRIAN S J · 2006 to 2019
$1.9M
Grp94-selective inhibitors to treat heredity glaucomaR01EY024232 · NEI · UNIVERSITY OF SOUTH FLORIDA · PI BLAGG, BRIAN S J, DESCHENES, ROBERT J · 2014 to 2017
$1.7M
Development of Hsp90 inhibitors for the treatment of cancerR01CA167079 · NCI · UNIVERSITY OF NOTRE DAME · PI BLAGG, BRIAN S J · 2012 to 2016
$1.5M
NCI NIH HHS CA120458NCI NIH HHS R01 CA120458NCI NIH HHS R01 CA167079NCI NIH HHS U01 CA120458NEI NIH HHS R01 EY024232
6 · The paper itself

Abstract

Modulation of Hsp90 C-terminal function represents a promising therapeutic approach for the treatment of cancer and neurodegenerative diseases. Current drug discovery efforts toward Hsp90 C-terminal inhibition focus on novobiocin, an antibiotic that was transformed into an Hsp90 inhibitor. Based on structural information obtained during the development of novobiocin derivatives and molecular docking studies, scaffolds containing a biphenyl moiety in lieu of the coumarin ring present in novobiocin were identified as new Hsp90 C-terminal inhibitors. Structure-activity relationship studies produced new derivatives that inhibit the proliferation of breast cancer cell lines at nanomolar concentrations, which corresponded directly with Hsp90 inhibition.

Indexed as

Drug DesignAntineoplastic AgentsBenzamidesBinding SitesBiphenyl CompoundsBlotting, WesternCell ProliferationHSP90 Heat-Shock ProteinsHumansMCF-7 CellsMolecular Docking SimulationMolecular StructureStructure-Activity RelationshipAntineoplastic AgentsBenzamidesBiphenyl CompoundsHSP90 Heat-Shock ProteinsBiphenylBreast cancerHeat shock protein 90Hsp90 C-Terminal inhibitorsStructure–activity relationship

Identifiers

PMID25462258
PMCPMC4406240
OpenAlexW2013431834

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.