Evidence map›Paper›PMID 29034069›Full record

ArticleMedChemComm2017

Scaffold hopping via ANCHOR.QUERY: β-lactams as potent p53-MDM2 antagonists

S Shaabani, C G Neochoritis, A Twarda-Clapa, B Musielak, T A Holak, A Dömling

Open access · hybridAbstract read
In one paragraph

Article in MedChemComm, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.

0numbers the graph read from it
0cells of the map it votes in
12citing papers in PubMed
1.8field-weighted citation impact, top 16% 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

12 citing papers in PubMed, 25 citations in OpenAlex.

  1. Article
  2. Article
  3. Article
  4. Article
  5. The Groebke-Blackburn-Bienaymé Reaction.European journal of chemistry (Print) · 2019
    Article
  6. Article
  7. Review
  8. Design of indole- and MCR-based macrocycles as p53-MDM2 antagonists.Beilstein journal of organic chemistry · 2019
    Article
  9. Artificial Macrocycles.Synlett : accounts and rapid communications in synthetic organic chemistry · 2018
    Article
  10. Article
  11. Artificial Macrocycles as Potent p53-MDM2 Inhibitors.ACS medicinal chemistry letters · 2017
    Article
  12. 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 2 institutions in 4 countries.

S ShaabaniDepartment of Drug Design, University of Groningen, The Netherlands.
C G NeochoritisDepartment of Drug Design, University of Groningen, The Netherlands.
A Twarda-ClapaFaculty of Biochemistry, Biophysics and Biotechnology, Jagiellonian University, Krakow, Poland.
B MusielakDepartment of Chemistry, Jagiellonian University, Krakow, Poland.
T A HolakFaculty of Biochemistry, Biophysics and Biotechnology, Jagiellonian University, Krakow, Poland.
A DömlingDepartment of Drug Design, University of Groningen, The Netherlands.
Jagiellonian University · PLUniversity of Groningen · NL

Funding

Real-time discovery of inhibitors among billion compounds for preview and downloadR01GM097082 · NIGMS · UNIVERSITY OF PITTSBURGH AT PITTSBURGH · PI CAMACHO, CARLOS J. · 2011 to 2020
$2.5M
NIGMS NIH HHS R01 GM097082
6 · The paper itself

Abstract

Using the pharmacophore-based virtual screening platform ANCHOR.QUERY, we morphed our recently described Ugi-4CR scaffold towards a β-lactam scaffold with potent p53-MDM2 antagonizing activities. 2D-HSQC and FP measurements confirm potent MDM2 binding. Molecular modeling studies are used to understand the observed SAR in the β-lactam series.

Identifiers

PMID29034069
PMCPMC5637554
OpenAlexW2600080366

What OpenQuestion holds

Textmetadata
LicenceTDM
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.