Evidence map›Paper›PMID 33502811›Full record

ArticleChemistry (Weinheim an der Bergstrasse, Germany)2021

Function-Oriented and Modular (+/-)-cis-Pseudoguaianolide Synthesis: Discovery of New Nrf2 Activators and NF-κB Inhibitors.

Fabien Emmetiere, Ranjala Ratnayake, Henry A M Schares, Katherine F M Jones, Emily Bevan-Smith, Hendrik Luesch, Daniel A Harki, Alexander J Grenning

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Chemistry (Weinheim an der Bergstrasse, Germany), 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing 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

5 citing papers in PubMed.

  1. Article
  2. Article
  3. Article
  4. Article
  5. 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

8 authors.

Fabien EmmetiereDepartment of Chemistry, University of Florida, PO Box 117200, Gainesville, FL, 32608, USA.
Ranjala RatnayakeDepartment of Medicinal Chemistry and Center for Natural Products, Drug Discovery and Development (CNPD3), University of Florida, Gainesville, FL, 32610, USA.
Henry A M ScharesDepartment of Medicinal Chemistry, University of Minnesota, Minneapolis, MN, 55455, USA.
Katherine F M JonesDepartment of Chemistry, University of Minnesota, Minneapolis, MN, 55455, USA.
Emily Bevan-SmithDepartment of Chemistry, University of Florida, PO Box 117200, Gainesville, FL, 32608, USA.
Hendrik LueschDepartment of Medicinal Chemistry and Center for Natural Products, Drug Discovery and Development (CNPD3), University of Florida, Gainesville, FL, 32610, USA.
Daniel A HarkiDepartment of Medicinal Chemistry, University of Minnesota, Minneapolis, MN, 55455, USA.
Alexander J GrenningDepartment of Chemistry, University of Florida, PO Box 117200, Gainesville, FL, 32608, USA.ORCID http://orcid.org/0000-0002-8182-9464

Funding

Novel Targeted Anticancer Agents from Marine CyanobacteriaR01CA172310 · NCI · UNIVERSITY OF FLORIDA · PI HENDRIK LUESCH · 2013 to 2026
$5.8M
Chemical Interrogation of Human DNA Cytosine DeaminasesR01GM110129 · NIGMS · UNIVERSITY OF MINNESOTA · PI HARKI, DANIEL A · 2015 to 2019
$1.8M
Acquisition of a Q Exactive HF Hybrid Quadrupole-OrbitrapS10OD021758 · OD · UNIVERSITY OF FLORIDA · PI BASSO, KARI B · 2017 to 2017
$600k
Development of Complex Natural Product Libraries and Multidimensional Anticancer Screening PlatformsR50CA211487 · NCI · UNIVERSITY OF FLORIDA · PI RATNAYAKE, RANJALA · 2016 to 2020
$440k
Directorate for Mathematical and Physical Sciences 1844443NCI NIH HHS R01 CA172310NCI NIH HHS R01CA172310NCI NIH HHS R50 CA211487NCI NIH HHS R50CA211487NIGMS NIH HHS R01 GM110129NIGMS NIH HHS R01GM110129NIH HHS S10 OD021758
6 · The paper itself

Abstract

Described herein is a function-oriented synthesis route and biological evaluation of pseudoguaianolide analogues. The 10-step synthetic route developed retains the topological complexity of the natural product, installs functional handles for late-stage diversification, and forges the key bioactive Michael acceptors early in the synthesis. The analogues were found to be low-micromolar Nrf2 activators and micromolar NF-κB inhibitors and dependent on the local environment of the Michael acceptor moieties.

Indexed as

Biological ProductsNF-E2-Related Factor 2NF-kappa BBiological ProductsNF-E2-Related Factor 2NF-kappa Benyne metathesismodular synthesisNF-κB inhibitorsNrf2 activatorspseudoguaianolides

Identifiers

PMID33502811
PMCPMC8195264

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.