Evidence map›Paper›PMID 31761657›Full record

ArticleBioorganic & medicinal chemistry letters2020

Inhibition of hedgehog signaling by stereochemically defined des-triazole itraconazole analogues.

Jiachen Wen, Kelly A Teske, M Kyle Hadden

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2020. 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. Transient Formation of Hemiketals from Pentafluoro-Journal of fluorine chemistry · 2023
    Article
  2. Molecules (Basel, Switzerland) · 2022
    Article
  3. Review
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

3 authors.

Jiachen WenDepartment of Pharmaceutical Sciences, University of Connecticut, 69 North Eagleville Rd, Unit 3092, Storrs, CT 06029-3092, United States.
Kelly A TeskeDepartment of Pharmaceutical Sciences, University of Connecticut, 69 North Eagleville Rd, Unit 3092, Storrs, CT 06029-3092, United States.
M Kyle HaddenDepartment of Pharmaceutical Sciences, University of Connecticut, 69 North Eagleville Rd, Unit 3092, Storrs, CT 06029-3092, United States. Electronic address: kyle.hadden@uconn.edu.

Funding

Itraconazole Analogues to Treat MedulloblastomaR01CA190617 · NCI · UNIVERSITY OF CONNECTICUT STORRS · PI HADDEN, MATTHEW KYLE · 2015 to 2019
$1.9M
NCI NIH HHS R01 CA190617
6 · The paper itself

Abstract

Dysregulation of the hedgehog (Hh) signaling pathway is associated with cancer occurrence and development in various malignancies. Previous structure-activity relationships (SAR) studies have provided potent Itraconazole (ITZ) analogues as Hh pathway antagonists. To further expand on our SAR for the ITZ scaffold, we synthesized and evaluated a series of compounds focused on replacing the triazole. Our results demonstrate that the triazole region is amenable to modification to a variety of different moieties; with a single methyl group representing the most favorable substituent. In addition, nonpolar substituents were more active than polar substituents. These SAR results provide valuable insight into the continued exploration of ITZ analogues as Hh pathway antagonists.

Indexed as

Hedgehog ProteinsHumansInhibitory Concentration 50ItraconazoleSignal TransductionStructure-Activity RelationshipTriazolesHedgehog ProteinsItraconazoleTriazolesHedgehog pathwayItraconazoleStructure-activity relationship

Identifiers

PMID31761657
PMCPMC6942223

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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.