Evidence map›Paper›PMID 27322235›Full record

ArticleMolecules (Basel, Switzerland)2016

Synthesis of Bioactive 2-(Arylamino)thiazolo[5,4-f]-quinazolin-9-ones via the Hügershoff Reaction or Cu- Catalyzed Intramolecular C-S Bond Formation.

Damien Hédou, Carole Dubouilh-Benard, Nadège Loaëc, Laurent Meijer, Corinne Fruit, Thierry Besson

Open access · goldAbstract 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 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
1.1field-weighted citation impact, top 19% 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

4 citing papers in PubMed, 7 citations in OpenAlex.

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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

6 authors at 3 institutions in 1 country.

Damien HédouNormandie Univ, UNIROUEN, INSA Rouen, CNRS, COBRA, 76000 Rouen, France. d.hedou@laposte.net.
Carole Dubouilh-BenardNormandie Univ, UNIROUEN, INSA Rouen, CNRS, COBRA, 76000 Rouen, France. carole.dubouilh@univ-rouen.fr.
Nadège LoaëcProtein Phosphorylation & Human Disease group, Station Biologique, 29680 Roscoff, France. Nadege.Loaec@univ-brest.fr.
Laurent MeijerManros Therapeutics, Centre de Perharidy, 29680 Roscoff, France. meijer@manros-therapeutics.com.
Corinne FruitNormandie Univ, UNIROUEN, INSA Rouen, CNRS, COBRA, 76000 Rouen, France. corinne.fruit@univ-rouen.fr.
Thierry BessonNormandie Univ, UNIROUEN, INSA Rouen, CNRS, COBRA, 76000 Rouen, France. thierry.besson@univ-rouen.fr.
Centre National de la Recherche Scientifique · FRManRos Therapeutics (France) · FRStation Biologique de Roscoff · FR

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

A library of thirty eight novel thiazolo[5,4-f]quinazolin-9(8H)-one derivatives (series 8, 10, 14 and 17) was prepared via the Hügershoff reaction and a Cu catalyzed intramolecular C-S bond formation, helped by microwave-assisted technology when required. The efficient multistep synthesis of the key 6-amino-3-cyclopropylquinazolin-4(3H)-one (3) has been reinvestigated and performed on a multigram scale from the starting 5-nitroanthranilic acid. The inhibitory potency of the final products was evaluated against five kinases involved in Alzheimer's disease and showed that some molecules of the 17 series described in this paper are particularly promising for the development of novel multi-target inhibitors of kinases.

Indexed as

Alzheimer DiseaseBarbituratesCatalysisCopperHumansMolecular StructureProtein Kinase InhibitorsQuinazolinonesStructure-Activity Relationship4-hydroxyquinazoline5-nitrobarbituric acidBarbituratesCopperProtein Kinase InhibitorsQuinazolinonesCDK5CK1CLK1DYRK1AGSK-3Hügershoff reactionmicrowave-assisted synthesisprotein kinasesthiazolo[5,4-f]quinazolin-9(8H)-ones

Identifiers

PMID27322235
PMCPMC6272913
OpenAlexW2431449931

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.