Evidence map›Paper›PMID 29487300›Full record

ArticleScientific reports2018

Rational Design, Synthesis and Biological Evaluation of Pyrimidine-4,6-diamine derivatives as Type-II inhibitors of FLT3 Selective Against c-KIT.

Jaideep B Bharate, Nicholas McConnell, Gunaganti Naresh, Lingtian Zhang, Naga Rajiv Lakkaniga, Lucky Ding, Neil P Shah, Brendan Frett, Hong-Yu Li

Open access · goldAbstract read
In one paragraph

Article in Scientific reports, 2018. 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 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

7 citing papers in PubMed, 17 citations in OpenAlex.

  1. Review
  2. Review
  3. Article
  4. Article
  5. Molecular Modeling Studies ofInternational journal of molecular sciences · 2021
    Article
  6. Article
  7. 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

9 authors at 4 institutions in 1 country.

Jaideep B BharateDepartment of Pharmaceutical Sciences, University of Arkansas for Medical Sciences, Little Rock, 72205, USA.
Nicholas McConnellDepartment of Pharmaceutical Sciences, University of Arkansas for Medical Sciences, Little Rock, 72205, USA.
Gunaganti NareshDepartment of Pharmaceutical Sciences, University of Arkansas for Medical Sciences, Little Rock, 72205, USA.
Lingtian ZhangDepartment of Pharmaceutical Sciences, University of Arkansas for Medical Sciences, Little Rock, 72205, USA.
Naga Rajiv LakkanigaDepartment of Pharmaceutical Sciences, University of Arkansas for Medical Sciences, Little Rock, 72205, USA.
Lucky DingDivision of Hematology/Oncology, University of California, San Francisco, CA, 94143, USA.
Neil P ShahDivision of Hematology/Oncology, University of California, San Francisco, CA, 94143, USA.
Brendan FrettDepartment of Pharmaceutical Sciences, University of Arkansas for Medical Sciences, Little Rock, 72205, USA.
Hong-Yu LiDepartment of Pharmaceutical Sciences, University of Arkansas for Medical Sciences, Little Rock, 72205, USA. HLi2@uams.edu.
University of Arkansas for Medical Sciences · USUCSF Helen Diller Family Comprehensive Cancer Center · USUniversity of Arizona · USUniversity of California, San Francisco · US

Funding

The Role o f Tetrahydrobiopterin (BH4) Bioavailability in Radiation-induced Skin InjuryP20GM109005 · NIGMS · UNIV OF ARKANSAS FOR MED SCIS · PI BOERMA, MARJAN · 2015 to 2024
$21.1M
Discovery and Development of a Selective pan-FLT3-ITD Kinase Inhibitor Clinical Candidate for the Treatment of FLT3-ITD-Driven AMLR01CA194094 · NCI · UNIV OF ARKANSAS FOR MED SCIS · PI LI, HONG-YU, SHAH, NEIL P · 2015 to 2018
$1.5M
NCI NIH HHS R01 CA194094NIGMS NIH HHS P20 GM109005
6 · The paper itself

Abstract

FMS-like Tyrosine Kinase 3 (FLT3) is a clinically validated target for acute myeloid leukemia (AML). Inhibitors targeting FLT3 have been evaluated in clinical studies and have exhibited potential to treat FLT3-driven AML. A frequent, clinical limitation is FLT3 selectivity, as concomitant inhibition of FLT3 and c-KIT is thought to cause dose-limiting myelosuppression. Through a rational design approach, novel FLT3 inhibitors were synthesized employing a pyridine/pyrimidine warhead. The most potent compound identified from the studies is compound 13a, which exhibited an IC

Indexed as

Antineoplastic AgentsCell Line, TumorEnzyme Activationfms-Like Tyrosine Kinase 3HumansProtein Kinase InhibitorsProto-Oncogene Proteins c-kitPyrimidinesStructure-Activity RelationshipAntineoplastic Agentsfms-Like Tyrosine Kinase 3Protein Kinase InhibitorsProto-Oncogene Proteins c-kitPyrimidines

Identifiers

PMID29487300
PMCPMC5829162
OpenAlexW2805625456

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.