Evidence map›Paper›PMID 28844386›Full record

ArticleBioorganic & medicinal chemistry letters2017

Modified biphenyl Hsp90 C-terminal inhibitors for the treatment of cancer.

Leah K Forsberg, Weiya Liu, Jeffrey Holzbeierlein, Brian S J Blagg

Open access · greenAbstract read
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
0.9field-weighted citation impact, top 26% 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

3 citing papers in PubMed, 14 citations in OpenAlex.

  1. Article
  2. Polθ Inhibition: An Anticancer Therapy for HR-Deficient Tumours.International journal of molecular sciences · 2022
    Review
  3. General Structural and Functional Features of Molecular Chaperones.Advances in experimental medicine and biology · 2021
    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

4 authors at 2 institutions in 1 country.

Leah K ForsbergDepartment of Medicinal Chemistry, 1251 Wescoe Hall Drive, Malott 4070, The University of Kansas, Lawrence, Kansas 66045-7563, United States.
Weiya LiuDepartment of Urology, 3901 Rainbow Boulevard, Stop 3016, The University of Kansas Medical Center, Kansas City, Kansas 66160, United States.
Jeffrey HolzbeierleinDepartment of Urology, 3901 Rainbow Boulevard, Stop 3016, The University of Kansas Medical Center, Kansas City, Kansas 66160, United States.
Brian S J BlaggDepartment of Medicinal Chemistry, 1251 Wescoe Hall Drive, Malott 4070, The University of Kansas, Lawrence, Kansas 66045-7563, United States. Electronic address: bblagg@ku.edu.
University of Kansas · USUniversity of Kansas Medical Center · US

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
The Role of Envelope in Heterosexual Transmission of HIVF32AI067079 · NIAID · EMORY UNIVERSITY · PI ALEXANDER, MELISSA A · 2005 to 2005
$44k
NCI NIH HHS R01 CA120458NCI NIH HHS U01 CA120458NIAID NIH HHS F32 AI067079
6 · The paper itself

Abstract

Heat Shock Protein 90 (Hsp90) is a molecular chaperone under clinical investigation for the treatment of neurodegenerative diseases and cancer. Neuroprotective Hsp90 C-terminal inhibitors (novologues) contain a biaryl ring system, and include KU-596, which was modified and investigated for potential anti-cancer activity. Incorporation of a benzamide group onto the biaryl novologues in lieu of the acetamide yielded compounds that manifest anti-cancer activity. Further exploration of the central phenyl ring led to compounds with enhanced anti-proliferative activity. The design, synthesis, and evaluation of these new analogs against breast and prostate cancer cell lines is reported herein, where it was found that 8b and 10 manifest potent anti-proliferative activity and a robust degradation of Hsp90 client-dependent proteins.

Indexed as

Antineoplastic AgentsBiphenyl CompoundsCell Line, TumorCell ProliferationDose-Response Relationship, DrugDrug Screening Assays, AntitumorHSP90 Heat-Shock ProteinsHumansModels, MolecularMolecular StructureStructure-Activity RelationshipAntineoplastic AgentsbiphenylBiphenyl CompoundsHSP90 Heat-Shock ProteinsBreast cancerHeat Shock Protein 90Hsp90 inhibitorsNovobiocin analogsProstate cancer

Identifiers

PMID28844386
PMCPMC5876719
OpenAlexW2734609837

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.