Evidence map›Paper›PMID 31425908›Full record

ArticleEuropean journal of medicinal chemistry2019

Novel derivatives of anaplastic lymphoma kinase inhibitors: Synthesis, radiolabeling, and preliminary biological studies of fluoroethyl analogues of crizotinib, alectinib, and ceritinib.

Bhasker Radaram, Federica Pisaneschi, Yi Rao, Ping Yang, David Piwnica-Worms, Mian M Alauddin

Open access · greenAbstract read
In one paragraph

Article in European journal of medicinal chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.

0numbers the graph read from it
0cells of the map it votes in
11citing papers in PubMed
0.3field-weighted citation impact, top 35% 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

11 citing papers in PubMed, 2 citations in OpenAlex.

  1. Review
  2. Review
  3. Review
  4. Review
  5. The blood-brain barrier: structure, regulation, and drug delivery.Signal transduction and targeted therapy · 2023
    Review
  6. Evaluation ofACS omega · 2023
    Article
  7. Review
  8. Recent advances in drug delivery and targeting to the brain.Journal of controlled release : official journal of the Controlled Release Society · 2022
    Review
  9. Concomitant mutation status ofTranslational lung cancer research · 2021
    Article
  10. N-[Bioorganic & medicinal chemistry letters · 2020
    Article
  11. 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

6 authors at 1 institution in 1 country.

Bhasker RadaramDepartment of Cancer Systems Imaging, The University of Texas MD Anderson Cancer Center, Houston, TX, 77030, USA.
Federica PisaneschiDepartment of Cancer Systems Imaging, The University of Texas MD Anderson Cancer Center, Houston, TX, 77030, USA.
Yi RaoDepartment of Cancer Systems Imaging, The University of Texas MD Anderson Cancer Center, Houston, TX, 77030, USA.
Ping YangDepartment of Cancer Systems Imaging, The University of Texas MD Anderson Cancer Center, Houston, TX, 77030, USA.
David Piwnica-WormsDepartment of Cancer Systems Imaging, The University of Texas MD Anderson Cancer Center, Houston, TX, 77030, USA. Electronic address: dpiwnica-worms@mdanderson.org.
Mian M AlauddinDepartment of Cancer Systems Imaging, The University of Texas MD Anderson Cancer Center, Houston, TX, 77030, USA. Electronic address: alauddin@mdanderson.org.
The University of Texas MD Anderson Cancer Center · US

Funding

Tumor Evolution and Metastasis ProgramP30CA016672 · NCI · UNIVERSITY OF TX MD ANDERSON CAN CTR · PI Fabien Delerue · 1985 to 2026
$290.8M
WU-MDACC Inter-Institutional Molecular Imaging CenterP50CA094056 · NCI · WASHINGTON UNIVERSITY · PI PIWNICA-WORMS, DAVID · 2002 to 2016
$26.3M
NCI NIH HHS P30 CA016672NCI NIH HHS P50 CA094056
6 · The paper itself

Abstract

Anaplastic lymphoma kinase (ALK), an oncogenic receptor tyrosine kinase, is a therapeutic target in various cancers, including non-small cell lung cancer. Although several ALK inhibitors, including crizotinib, ceritinib, and alectinib, are approved for cancer treatment, their long-term benefit is often limited by the cancer's acquisition of resistance owing to secondary point mutations in ALK. Importantly, some ALK inhibitors cannot cross the blood-brain barrier (BBB) and thus have little or no efficacy against brain metastases. The introduction of a lipophilic moiety, such as a fluoroethyl group may improve the drug's BBB penetration. Herein, we report the synthesis of fluoroethyl analogues of crizotinib 1, alectinib 4, and ceritinib 9, and their radiolabeling with

Indexed as

Anaplastic Lymphoma KinaseAnimalsAntineoplastic AgentsCarbazolesCell Line, TumorCell ProliferationCrizotinibDose-Response Relationship, DrugDrug Screening Assays, AntitumorFluorine RadioisotopesHumansMiceMolecular StructurePiperidinesPositron-Emission TomographyProtein Kinase InhibitorsalectinibAnaplastic Lymphoma KinaseAntineoplastic AgentsCarbazolesceritinibCrizotinibFluorine-18Fluorine RadioisotopesPiperidinesProtein Kinase InhibitorsPyrimidinesSulfonesAnaplastic lymphoma kinaseBrain metastasisLung cancerPETTargeted therapeutics

Identifiers

PMID31425908
PMCPMC7193943
OpenAlexW2948659304

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.