Evidence map›Paper›PMID 24953820›Full record

ArticleBioorganic & medicinal chemistry letters2014

Novologues containing a benzamide side chain manifest anti-proliferative activity against two breast cancer cell lines.

Huiping Zhao, Mercy Anyika, Antwan Girgis, Brian S J Blagg

Open access · bronzeAbstract read
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 8 papers.

0numbers the graph read from it
0cells of the map it votes in
8citing papers in PubMed
1.1field-weighted citation impact, top 22% 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

8 citing papers in PubMed, 16 citations in OpenAlex.

  1. Review
  2. The heat shock response and small molecule regulators.European journal of medicinal chemistry · 2021
    Review
  3. Article
  4. Article
  5. Article
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  7. Review
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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

4 authors at 1 institution in 1 country.

Huiping ZhaoDepartment of Medicinal Chemistry, The University of Kansas, 1251 Wescoe Hall Drive, Malott 4070, Lawrence, KS 66045-7563, United States.
Mercy AnyikaDepartment of Medicinal Chemistry, The University of Kansas, 1251 Wescoe Hall Drive, Malott 4070, Lawrence, KS 66045-7563, United States.
Antwan GirgisDepartment of Medicinal Chemistry, The University of Kansas, 1251 Wescoe Hall Drive, Malott 4070, Lawrence, KS 66045-7563, United States.
Brian S J BlaggDepartment of Medicinal Chemistry, The University of Kansas, 1251 Wescoe Hall Drive, Malott 4070, Lawrence, KS 66045-7563, United States. Electronic address: bblagg@ku.edu.
University of Kansas · US

Funding

Chaperone therapeutics for the treatment of DPNR01NS075311 · NINDS · UNIVERSITY OF NOTRE DAME · PI BLAGG, BRIAN S J, DOBROWSKY, RICK T · 2012 to 2020
$2.8M
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
NCI NIH HHS CA120458NCI NIH HHS U01 CA120458NINDS NIH HHS NS075311NINDS NIH HHS R01 NS075311
6 · The paper itself

Abstract

Hsp90 represents a promising target for the development of both anti-cancer and neuroprotective agents. Structure-activity relationship studies on novobiocin and novobiocin analogues, led to the development of KU-32 and recently, KU-596, as lead compounds for the potential treatment of neurodegenerative diseases. Similar to KU-32, we have demonstrated that upon replacement of the acetamide side chain present in KU-32 with a benzamide, this neuroprotective agent was transformed into a scaffold that manifests anti-proliferative activity. To assess structure-activity relationships for this new scaffold, a library of benzamide-containing novologues was prepared and evaluated against two breast cancer cell lines. Compound 14a manifested the most potent anti-proliferative activity from these studies and induced Hsp90-dependent client protein degradation in a concentration-dependent manner.

Indexed as

Antineoplastic AgentsBenzamidesCell Line, TumorCell ProliferationDose-Response Relationship, DrugDrug Screening Assays, AntitumorHSP90 Heat-Shock ProteinsHumansMCF-7 CellsMolecular StructureStructure-Activity RelationshipAntineoplastic AgentsbenzamideBenzamidesHSP90 Heat-Shock ProteinsBreast cancerHeat shock protein 90Hsp90 inhibitorsNovobiocin analogues

Identifiers

PMID24953820
PMCPMC4096108
OpenAlexW2083030025

What OpenQuestion holds

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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.