Evidence map›Paper›PMID 27187326›Full record

ArticleMolecules (Basel, Switzerland)2016

Discovery of Potent c-MET Inhibitors with New Scaffold Having Different Quinazoline, Pyridine and Tetrahydro-Pyridothienopyrimidine Headgroups.

Yingnan Jiang, Ke Zhang, Suyu Gao, Guihua Wang, Jian Huang, Jinhui Wang, Lixia Chen

Abstract read
In one paragraph

Article in Molecules (Basel, Switzerland), 2016. 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
–field-weighted citation impact
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.

  1. Met Receptor Tyrosine Kinase and Chemoprevention of Oral Cancer.Journal of the National Cancer Institute · 2018
    Trial
  2. Article
  3. Article
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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

7 authors.

Yingnan JiangSchool of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, China. j1074736705@163.com.
Ke ZhangSchool of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, China. xjzk1984@163.com.
Suyu GaoSchool of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, China. gsy19900922@163.com.
Guihua WangSchool of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, China. redticky@126.com.
Jian HuangSchool of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, China. 13504051049@163.com.
Jinhui WangSchool of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, China. profwjh@126.com.
Lixia ChenSchool of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, China. syzyclx@163.com.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Cellular mesenchymal-epithelial transition factor (c-MET) is closely linked to human malignancies, which makes it an important target for treatment of cancer. In this study, a series of 3-methoxy-N-phenylbenzamide derivatives, N-(3-(tert-butyl)-1-phenyl-1H-pyrazol-5-yl) benzamide derivatives and N¹-(3-fluoro-4-methoxyphenyl)-N³-(4-fluorophenyl) malonamide derivatives were designed and synthesized, some of them were identified as c-MET inhibitors. Among these compounds with new scaffolds having different quinazoline, pyridine and tetrahydro-pyridothienopyrimidine head groups, compound 11c, 11i, 13b, 13h exhibited both potent inhibitory activities against c-MET and high anticancer activity against tested cancer cell lines in vitro. In addition, kinase selectivity assay further demonstrated that both 13b and 13h are potent and selective c-MET inhibitors. Molecular docking supported that they bound well to c-MET and VEGFR2, which demonstrates that they are potential c-MET RTK inhibitors for cancer therapy.

Indexed as

Drug DiscoveryCell Line, TumorCell ProliferationHumansMagnetic Resonance SpectroscopyMass SpectrometryModels, MolecularProtein Kinase InhibitorsProto-Oncogene Proteins c-metPyridinesQuinazolinesStructure-Activity RelationshipProtein Kinase InhibitorsProto-Oncogene Proteins c-metPyridinesQuinazolinescancer therapyMET inhibitorpyridinequinazolinetetrahydro-pyridothienopyrimidine

Identifiers

PMID27187326
PMCPMC6272887

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.