Evidence map›Paper›PMID 27173800›Full record

ArticleBioorganic & medicinal chemistry letters2016

Identification of quinones as novel PIM1 kinase inhibitors.

Richard L Schroeder, Navneet Goyal, Melyssa Bratton, Ian Townley, Nancy A Pham, Phan Tram, Treasure Stone, Jasmine Geathers, Kathy Nguyen, Jayalakshmi Sridhar

Open access · greenAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2016. 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
2.0field-weighted citation impact, top 15% 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, 14 citations in OpenAlex.

  1. Crystal structure of 4-bromo-5,7-dimeth-oxy-2,3-di-hydro-1Acta crystallographica. Section E, Crystallographic communications · 2024
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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 1 institution in 1 country.

Richard L SchroederDepartment of Chemistry, Xavier University of Louisiana, 1, Drexel Dr., New Orleans, LA 70125, USA.
Navneet GoyalDepartment of Chemistry, Xavier University of Louisiana, 1, Drexel Dr., New Orleans, LA 70125, USA.
Melyssa BrattonCell and Molecular Biology Core Facility, Xavier University of Louisiana, New Orleans, LA 70125, USA.
Ian TownleyCell and Molecular Biology Core Facility, Xavier University of Louisiana, New Orleans, LA 70125, USA.
Nancy A PhamDepartment of Chemistry, Xavier University of Louisiana, 1, Drexel Dr., New Orleans, LA 70125, USA.
Phan TramDepartment of Chemistry, Xavier University of Louisiana, 1, Drexel Dr., New Orleans, LA 70125, USA.
Treasure StoneDepartment of Chemistry, Xavier University of Louisiana, 1, Drexel Dr., New Orleans, LA 70125, USA.
Jasmine GeathersDepartment of Chemistry, Xavier University of Louisiana, 1, Drexel Dr., New Orleans, LA 70125, USA.
Kathy NguyenDepartment of Chemistry, Xavier University of Louisiana, 1, Drexel Dr., New Orleans, LA 70125, USA.
Jayalakshmi SridharDepartment of Chemistry, Xavier University of Louisiana, 1, Drexel Dr., New Orleans, LA 70125, USA. Electronic address: jsridhar@xula.edu.
Xavier University of Louisiana · US

Funding

STABILITY' (symptomatic review during biologic therapy) Review in Inflammatory Bowel DiseaseP20GM103424 · NIGMS · LOUISIANA STATE UNIV A&M COL BATON ROUGE · PI Konstantin G Kousoulas · 2012 to 2026
$57.4M
Xavier's RCMI Cancer Research ProgramG12MD007595 · NIMHD · XAVIER UNIVERSITY OF LOUISIANA · PI D'AMOUR, GENE, WANG, GUANGDI · 2012 to 2018
$15.7M
Building Integrated Pathways to Independence for Diverse Biomedical ResearchersUL1MD009607 · NIMHD · XAVIER UNIVERSITY OF LOUISIANA · PI D'AMOUR, GENE · 2014 to 2014
$2.2M
NIGMS NIH HHS P20 GM103424NIMHD NIH HHS G12 MD007595NIMHD NIH HHS UL1 MD009607
6 · The paper itself

Abstract

PIM1 is a proto-oncogene encoding the serine/threonine PIM1 kinase. PIM1 kinase plays important roles in regulating aspects of cell cycle progression, apoptosis resistance, and has been implicated in the development of such malignancies as prostate cancer and acute myeloid leukemia among others. Knockout of PIM1 kinase in mice has been shown to be non-lethal without any obvious phenotypic changes, making it an attractive therapeutic target. Our investigation of anthraquinones as kinase inhibitors revealed a series of quinone analogs showing high selectivity for inhibition of the PIM kinases. Molecular modeling studies were used to identify key interactions and binding poses of these compounds within the PIM1 binding pocket. Compounds 1, 4, 7 and 9 inhibited the growth of DU-145 prostate cancer cell lines with a potency of 8.21μM, 4.06μM, 3.21μM and 2.02μM.

Indexed as

Antineoplastic AgentsCell Line, TumorCell ProliferationDose-Response Relationship, DrugDrug Screening Assays, AntitumorHumansMaleMolecular StructureProstatic NeoplasmsProtein Kinase InhibitorsProto-Oncogene MasProto-Oncogene Proteins c-pim-1QuinonesStructure-Activity RelationshipAntineoplastic AgentsMAS1 protein, humanPIM1 protein, humanProtein Kinase InhibitorsProto-Oncogene MasProto-Oncogene Proteins c-pim-1QuinonesEmodinPim1 kinaseProstate cancerQuinonesSelectivity profile

Identifiers

PMID27173800
PMCPMC4899092
OpenAlexW2343925679

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.