Evidence map›Paper›PMID 33299257›Full record

ArticleTetrahedron2020

Aniline-containing derivatives of parthenolide: Synthesis and anti-chronic lymphocytic leukaemia activity.

Alex S Quy, Xingjian Li, Louise Male, Tatjana Stankovic, Angelo Agathanggelou, John S Fossey

Open access · hybridAbstract read
In one paragraph

Article in Tetrahedron, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
0.3field-weighted citation impact, top 42% 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

4 citing papers in PubMed, 10 citations in OpenAlex.

  1. Review
  2. Article
  3. Review
  4. 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

6 authors at 1 institution in 1 country.

Alex S QuySchool of Chemistry, University of Birmingham, Edgbaston, Birmingham, West Midlands, B15 2TT, UK.
Xingjian LiSchool of Chemistry, University of Birmingham, Edgbaston, Birmingham, West Midlands, B15 2TT, UK.
Louise MaleX-Ray Crystallography Facility, School of Chemistry, University of Birmingham, Edgbaston, Birmingham, West Midlands, B15 2TT, UK.
Tatjana StankovicInstitute for Cancer and Genomic Sciences, University of Birmingham, Edgbaston, Birmingham, West Midlands, UK.
Angelo AgathanggelouInstitute for Cancer and Genomic Sciences, University of Birmingham, Edgbaston, Birmingham, West Midlands, UK.
John S FosseySchool of Chemistry, University of Birmingham, Edgbaston, Birmingham, West Midlands, B15 2TT, UK.
University of Birmingham · GB

Funding

Cancer Research UK 20951Cancer Research UK 28640
6 · The paper itself

Abstract

Parthenolide exhibits anti-leukaemia activity, whilst its synthetic modification to impart improve drug-like properties, including 1,4-conjugate addition of primary and secondary amines, have previously been used, 1,4-addition of aniline derivatives to parthenolide has not been fully explored. A protocol for such additions to parthenolide is outlined herein. Reaction conditions were determined using tulipane as a model Michael acceptor. Subsequently, aniline-containing parthenolide derivatives were prepared under the optimised conditions and single crystal X-ray diffraction structures were resolved for three of the compounds synthesised. The synthesised derivatives, along with compounds resulting from a side reaction, were tested for their in vitro anti-leukaemia activity using the chronic lymphocytic leukaemia (CLL) MEC1 cell line. Computational studies with the 2RAM protein structure suggested that the activity of the derivatives was independent of their in silico ability to dock with the Cys38 residue of NF-κB.

Indexed as

1,4-Conjugate additionAnilineChronic lymphocytic leukaemia (CLL)LeukemiaNatural product derivativesParthenolide (PTL)

Identifiers

PMID33299257
PMCPMC7695678
OpenAlexW3092815593

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.