Evidence map›Paper›PMID 24387866›Full record

ArticleBioorganic & medicinal chemistry2014

Identifying novel targets in renal cell carcinoma: design and synthesis of affinity chromatography reagents.

Muriel Bonnet, Jack U Flanagan, Denise A Chan, Amato J Giaccia, Michael P Hay

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry, 2014. 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
–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

3 citing papers in PubMed.

  1. Permuted 2,4-thiazolidinedione (TZD) analogs as GLUT inhibitors and their in-vitro evaluation in leukemic cells.European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences · 2020
    Article
  2. Article
  3. 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.

Muriel BonnetAuckland Cancer Society Research Centre, The University of Auckland, Private Bag 92019, Auckland 1142, New Zealand.
Jack U FlanaganAuckland Cancer Society Research Centre, The University of Auckland, Private Bag 92019, Auckland 1142, New Zealand; Maurice Wilkins Centre for Molecular Biodiscovery, University of Auckland, Auckland, New Zealand.
Denise A ChanDepartment of Radiation Oncology, Stanford University School of Medicine, Stanford, CA 94305, USA.
Amato J GiacciaDepartment of Radiation Oncology, Stanford University School of Medicine, Stanford, CA 94305, USA.
Michael P HayAuckland Cancer Society Research Centre, The University of Auckland, Private Bag 92019, Auckland 1142, New Zealand; Maurice Wilkins Centre for Molecular Biodiscovery, University of Auckland, Auckland, New Zealand. Electronic address: m.hay@auckland.ac.nz.

Funding

TUMOR HYPOXIA--MOLECULAR STUDIES &CLINICAL EXPLOITATIONP01CA067166 · NCI · STANFORD UNIVERSITY · PI GIACCIA, AMATO J. · 1996 to 2017
$25.5M
Small-molecule Cytotoxics Dependent on HIF1 ActivityP01CA082566 · NCI · STANFORD UNIVERSITY · PI BOULEY, DONNA M. · 2000 to 2008
$8.0M
The Role of Hypoxia-inducible Factor-1alpha in TumorigenesisF32CA123823 · NCI · STANFORD UNIVERSITY · PI CHAN, DENISE A · 2006 to 2008
$151k
NCI NIH HHS CA-123823NCI NIH HHS CA-82566NCI NIH HHS F32 CA123823NCI NIH HHS P01 CA067166NCI NIH HHS P01 CA082566
6 · The paper itself

Abstract

Two novel scaffolds, 4-pyridylanilinothiazoles (PAT) and 3-pyridylphenylsulfonyl benzamides (PPB), previously identified as selective cytotoxins for von Hippel-Lindau-deficient Renal Carcinoma cells, were used as templates to prepare affinity chromatography reagents to aid the identification of the molecular targets of these two classes. Structure-activity data and computational models were used to predict possible points of attachment for linker chains. In the PAT class, Click coupling of long chain azides with 2- and 3-pyridylanilinothiazoleacetylenes gave triazole-linked pyridylanilinothiazoles which did not retain the VHL-dependent selectivity of parent analogues. For the PPB class, Sonagashira coupling of 4-iodo-(3-pyridylphenylsulfonyl)benzamide with a propargyl hexaethylene glycol carbamate gave an acetylene which was reduced to the corresponding alkyl 3-pyridylphenylsulfonylbenzamide. This reagent retained the VHL-dependent selectivity of the parent analogues and was successfully utilized as an affinity reagent.

Indexed as

Drug DesignAntineoplastic AgentsBenzamidesCarcinoma, Renal CellCell Line, TumorCell ProliferationChromatography, AffinityDose-Response Relationship, DrugDrug Screening Assays, AntitumorHumansKidney NeoplasmsModels, MolecularMolecular StructurePyridinesStructure-Activity RelationshipSulfones3-pyridylphenylsulfonyl benzamide4-pyridylanilinothiazoleAntineoplastic AgentsBenzamidesPyridinesSulfonesThiazolesBOCClick chemistryDCMdichloromethanedimethylformamideDMFGLUT-1high throughput screeningHTSPATPEGpolyethylene glycolPPBpyridylanilino thiazolepyridylphenylsulfonyl benzamidesRCCrenal cell carcinomaRenal cell carcinomaSARSonogashira cross couplingstructure–activity relationshipTBTAtert-butyloxycarbonyltetrahydrofuranTFATHFTMStrifluoroacetic acidtrimethylsilyltris-(benzyltriazolyl)amineVon Hippel–Lindau factor

Identifiers

PMID24387866
PMCPMC5713883

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.