Evidence map›Paper›PMID 28090282›Full record

ArticleMedChemComm2016

Traceless Solid-Phase α-Hydroxytropolone Synthesis.

Michael P D'Erasmo, Takashi Masaoka, Jennifer A Wilson, Errol M Hunte, John A Beutler, Stuart F J Le Grice, Ryan P Murelli

Abstract read
In one paragraph

Article in MedChemComm, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.

0numbers the graph read from it
0cells of the map it votes in
9citing 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

9 citing papers in PubMed.

  1. Article
  2. Article
  3. Article
  4. Article
  5. Article
  6. Fluorous-Phase Approach to α-Hydroxytropolone Synthesis.The Journal of organic chemistry · 2018
    Article
  7. Article
  8. Article
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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

7 authors.

Michael P D'ErasmoDepartment of Chemistry, Brooklyn College, The City University of New York, Brooklyn, New York, USA; PhD Program in Chemistry, The Graduate Center of The City University of New York, New York, NY, USA.
Takashi MasaokaBasic Research Laboratory, National Cancer Institute, Frederick, MD, USA.
Jennifer A WilsonMolecular Targets Laboratory, National Cancer Institute, Frederick, MD, USA.
Errol M HunteDepartment of Chemistry, Brooklyn College, The City University of New York, Brooklyn, New York, USA.
John A BeutlerMolecular Targets Laboratory, National Cancer Institute, Frederick, MD, USA.
Stuart F J Le GriceBasic Research Laboratory, National Cancer Institute, Frederick, MD, USA.
Ryan P MurelliDepartment of Chemistry, Brooklyn College, The City University of New York, Brooklyn, New York, USA; PhD Program in Chemistry, The Graduate Center of The City University of New York, New York, NY, USA.

Funding

Development and Exploitation of New Synthetic Strategies for TropolonesSC1GM111158 · NIGMS · BROOKLYN COLLEGE · PI MURELLI, RYAN · 2015 to 2023
$3.1M
NIGMS NIH HHS SC1 GM111158
6 · The paper itself

Abstract

α-Hydroxytropolones are established inhibitors of several therapeutically relevant binuclear metalloenzymes, and thus lead drug targets for various human diseases. We have leveraged a recently-disclosed three-component oxidopyrylium cycloaddition in the first solid-phase synthesis of α-hydroxytropolones. We also showed that, while minor impurities exist after cleavage and aqueous wash, the semi-crude products display activity in HIV RT-associated RNaseH enzymatic and cell-based assays consistent with pure molecules made in solution phase. These proof-of-principle studies demonstrate the feasibility of solid-phase α-hydroxytropolone synthesis and its potential to serve as a powerful platform for α-hydroxytropolone-based drug discovery and development.

Identifiers

PMID28090282
PMCPMC5228208

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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.