Evidence map›Paper›PMID 30460842›Full record

ArticleJournal of medicinal chemistry2018

Application of Sequential Palladium Catalysis for the Discovery of Janus Kinase Inhibitors in the Benzo[ c]pyrrolo[2,3- h][1,6]naphthyridin-5-one (BPN) Series.

Mohamed S A Elsayed, Jeffery J Nielsen, Sungtae Park, Jeongho Park, Qingyang Liu, Chang H Kim, Yves Pommier, Keli Agama, Philip S Low, Mark Cushman

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2018. 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
1.3field-weighted citation impact, top 24% 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

5 citing papers in PubMed, 20 citations in OpenAlex.

  1. Article
  2. Article
  3. Synthetic Routes to 2-aryl-1Molecules (Basel, Switzerland) · 2024
    Article
  4. Review
  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

10 authors at 2 institutions in 1 country.

Mohamed S A ElsayedDepartment of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy , Purdue University , West Lafayette , Indiana 47907 , United States.ORCID 0000-0002-1353-7259
Jeffery J NielsenDepartment of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy , Purdue University , West Lafayette , Indiana 47907 , United States.
Sungtae ParkDepartment of Comparative Pathobiology, College of Veterinary Medicine , Purdue University , West Lafayette , Indiana 47907 , United States.
Jeongho ParkDepartment of Comparative Pathobiology, College of Veterinary Medicine , Purdue University , West Lafayette , Indiana 47907 , United States.
Qingyang LiuDepartment of Comparative Pathobiology, College of Veterinary Medicine , Purdue University , West Lafayette , Indiana 47907 , United States.
Chang H KimDepartment of Comparative Pathobiology, College of Veterinary Medicine , Purdue University , West Lafayette , Indiana 47907 , United States.
Yves PommierDevelopmental Therapeutics Branch and Laboratory of Molecular Pharmacology, Center for Cancer Research , National Cancer Institute , Bethesda , Maryland 20892 , United States.
Keli AgamaDevelopmental Therapeutics Branch and Laboratory of Molecular Pharmacology, Center for Cancer Research , National Cancer Institute , Bethesda , Maryland 20892 , United States.
Philip S LowThe Purdue Center for Cancer Research , Purdue University , West Lafayette , Indiana 47907 , United States.ORCID 0000-0001-9042-5528
Mark CushmanDepartment of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy , Purdue University , West Lafayette , Indiana 47907 , United States.ORCID 0000-0002-0152-5891
Purdue University West Lafayette · USNational Cancer Institute · US

Funding

Transgenic Mouse Core Facility Shared Resource (TMCF-SR)P30CA023168 · NCI · PURDUE UNIVERSITY WEST LAFAYETTE · PI Andrea L Kasinski · 1985 to 2026
$43.4M
DNA Topoisomerases as Target of Action of Anticancer DrugsZIABC006161 · NCI · DIVISION OF BASIC SCIENCES - NCI · PI POMMIER, YVES · 2009 to 2025
$16.8M
Homing of Functionally Distinct ILC SubsetsR01AI121302 · NIAID · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI KIM, CHANG H · 2016 to 2020
$1.9M
DNA TOPOISOMERASES AS TARGET OF ACTION OF ANTICANCER DRUGSZ01BC006161 · NCI · DIVISION OF BASIC SCIENCES - NCI · PI POMMIER, YVES · 1996 to 2008
$1.5M
Migration and function of Th17 cells in the gutR01AI080769 · NIAID · PURDUE UNIVERSITY · PI KIM, CHANG H · 2010 to 2013
$1.3M
Intramural NIH HHS Z01 BC006161Intramural NIH HHS ZIA BC006161NCI NIH HHS P30 CA023168NIAID NIH HHS R01 AI080769NIAID NIH HHS R01 AI121302
6 · The paper itself

Abstract

The present account describes the discovery and development of a new benzo[ c]pyrrolo[2,3- h][1,6]naphthyridin-5-one (BPN) JAK inhibitory chemotype that has produced selective JAK inhibitors. Sequential palladium chemistry was optimized for the rapid access to a focused library of derivatives to explore the structure-activity relationships of the new scaffold. Several compounds from the series displayed potencies in the low nanomolar range against the four members of the JAK family with various selectivity profiles. Compound 20a, with an azetidine amide side chain, showed the best selectivity for JAK1 kinase vs JAK2, JAK3, and TYK2, with low nanomolar potency (IC

Indexed as

Drug DiscoveryCaco-2 CellsCatalysisHumansJanus Kinase InhibitorsJanus KinasesModels, MolecularPalladiumPermeabilityProtein ConformationPyrrolesTissue DistributionJanus Kinase InhibitorsJanus KinasesPalladiumPyrroles

Identifiers

PMID30460842
PMCPMC8142550
OpenAlexW2901909430

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.