Evidence map›Paper›PMID 25589931›Full record

ArticleACS medicinal chemistry letters2015

Pyrimidine-based tricyclic molecules as potent and orally efficacious inhibitors of wee1 kinase.

Yunsong Tong, Maricel Torrent, Alan S Florjancic, Kenneth D Bromberg, Fritz G Buchanan, Debra C Ferguson, Eric F Johnson, Loren M Lasko, David Maag, Philip J Merta and 5 more

Open access · greenAbstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.

0numbers the graph read from it
0cells of the map it votes in
7citing papers in PubMed
1.0field-weighted citation impact, top 25% 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

7 citing papers in PubMed, 19 citations in OpenAlex.

  1. Review
  2. Article
  3. Review
  4. Selective Wee1 Inhibitors Led to Antitumor ActivityACS medicinal chemistry letters · 2023
    Article
  5. Wee1 Kinase: A Potential Target to Overcome Tumor Resistance to Therapy.International journal of molecular sciences · 2021
    Review
  6. Review
  7. 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

15 authors at 2 institutions in 1 country.

Yunsong TongCancer Research, Molecular Modeling, Pharmacology, and High Throughput Biology, Research and Development, AbbVie , 1 North Waukegan Road, North Chicago, Illinois 60064-6114, United States.
Maricel TorrentCancer Research, Molecular Modeling, Pharmacology, and High Throughput Biology, Research and Development, AbbVie , 1 North Waukegan Road, North Chicago, Illinois 60064-6114, United States.
Alan S FlorjancicCancer Research, Molecular Modeling, Pharmacology, and High Throughput Biology, Research and Development, AbbVie , 1 North Waukegan Road, North Chicago, Illinois 60064-6114, United States.
Kenneth D BrombergCancer Research, Molecular Modeling, Pharmacology, and High Throughput Biology, Research and Development, AbbVie , 1 North Waukegan Road, North Chicago, Illinois 60064-6114, United States.
Fritz G BuchananCancer Research, Molecular Modeling, Pharmacology, and High Throughput Biology, Research and Development, AbbVie , 1 North Waukegan Road, North Chicago, Illinois 60064-6114, United States.
Debra C FergusonCancer Research, Molecular Modeling, Pharmacology, and High Throughput Biology, Research and Development, AbbVie , 1 North Waukegan Road, North Chicago, Illinois 60064-6114, United States.
Eric F JohnsonCancer Research, Molecular Modeling, Pharmacology, and High Throughput Biology, Research and Development, AbbVie , 1 North Waukegan Road, North Chicago, Illinois 60064-6114, United States.
Loren M LaskoCancer Research, Molecular Modeling, Pharmacology, and High Throughput Biology, Research and Development, AbbVie , 1 North Waukegan Road, North Chicago, Illinois 60064-6114, United States.
David MaagCancer Research, Molecular Modeling, Pharmacology, and High Throughput Biology, Research and Development, AbbVie , 1 North Waukegan Road, North Chicago, Illinois 60064-6114, United States.
Philip J MertaCancer Research, Molecular Modeling, Pharmacology, and High Throughput Biology, Research and Development, AbbVie , 1 North Waukegan Road, North Chicago, Illinois 60064-6114, United States.
Amanda M OlsonCancer Research, Molecular Modeling, Pharmacology, and High Throughput Biology, Research and Development, AbbVie , 1 North Waukegan Road, North Chicago, Illinois 60064-6114, United States.
Donald J OsterlingCancer Research, Molecular Modeling, Pharmacology, and High Throughput Biology, Research and Development, AbbVie , 1 North Waukegan Road, North Chicago, Illinois 60064-6114, United States.
Nirupama SoniCancer Research, Molecular Modeling, Pharmacology, and High Throughput Biology, Research and Development, AbbVie , 1 North Waukegan Road, North Chicago, Illinois 60064-6114, United States.
Alexander R ShoemakerCancer Research, Molecular Modeling, Pharmacology, and High Throughput Biology, Research and Development, AbbVie , 1 North Waukegan Road, North Chicago, Illinois 60064-6114, United States.
Thomas D PenningCancer Research, Molecular Modeling, Pharmacology, and High Throughput Biology, Research and Development, AbbVie , 1 North Waukegan Road, North Chicago, Illinois 60064-6114, United States.
AbbVie (United States) · USHigh Throughput Biology (United States) · US

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Aided by molecular modeling, compounds with a pyrimidine-based tricyclic scaffold were designed and confirmed to inhibit Wee1 kinase. Structure-activity studies identified key pharmacophores at the aminoaryl and halo-benzene regions responsible for binding affinity with sub-nM K i values. The potent inhibitors demonstrated sub-μM activities in both functional and mechanism-based cellular assays and also possessed desirable pharmacokinetic profiles. The lead molecule, 31, showed oral efficacy in potentiating the antiproliferative activity of irinotecan, a cytotoxic agent, in a NCI-H1299 mouse xenograft model.

Indexed as

antitumorWee1 kinase inhibitors

Identifiers

PMID25589931
PMCPMC4291713
OpenAlexW2315123131

What OpenQuestion holds

Textmetadata
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.