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dc.contributor.author
Larghi, Enrique Leandro  
dc.contributor.author
Bruneau, Alexandre  
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Sauvage, Félix  
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Alami, Mouad  
dc.contributor.author
Vergnaud-Gauduchon, Juliette  
dc.contributor.author
Messaoudi, Samir  
dc.date.available
2023-07-17T15:59:55Z  
dc.date.issued
2022-01-09  
dc.identifier.citation
Larghi, Enrique Leandro; Bruneau, Alexandre; Sauvage, Félix; Alami, Mouad; Vergnaud-Gauduchon, Juliette; et al.; Synthesis and Biological Activity of 3-(Heteroaryl)quinolin-2(1H)-ones Bis-Heterocycles as Potential Inhibitors of the Protein Folding Machinery Hsp90; Molecular Diversity Preservation International; Molecules; 27; 2; 9-1-2022; 1-13  
dc.identifier.issn
1420-3049  
dc.identifier.uri
http://hdl.handle.net/11336/204197  
dc.description.abstract
In the context of our SAR study concerning 6BrCaQ analogues as C-terminal Hsp90 inhibitors, we designed and synthesized a novel series of 3-(heteroaryl)quinolin-2(1H), of types 3, 4, and 5, as a novel class of analogues. A Pd-catalyzed Liebeskind–Srogl cross-coupling was developed as a convenient approach for easy access to complex purine architectures. This series of analogues showed a promising biological effect against MDA-MB231 and PC-3 cancer cell lines. This study led to the identification of the best compounds, 3b (IC50 = 28 µM) and 4e, which induce a significant decrease of CDK-1 client protein and stabilize the levels of Hsp90 and Hsp70 without triggering the HSR response.  
dc.format
application/pdf  
dc.language.iso
eng  
dc.publisher
Molecular Diversity Preservation International  
dc.rights
info:eu-repo/semantics/openAccess  
dc.rights.uri
https://creativecommons.org/licenses/by/2.5/ar/  
dc.subject
3-(HETEROARYL)QUINOLIN-2(1H)-ONES  
dc.subject
6BRCAQ  
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CYTOTOXICITY  
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HSP90  
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PURINES  
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Química Orgánica  
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Ciencias Químicas  
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CIENCIAS NATURALES Y EXACTAS  
dc.title
Synthesis and Biological Activity of 3-(Heteroaryl)quinolin-2(1H)-ones Bis-Heterocycles as Potential Inhibitors of the Protein Folding Machinery Hsp90  
dc.type
info:eu-repo/semantics/article  
dc.type
info:ar-repo/semantics/artículo  
dc.type
info:eu-repo/semantics/publishedVersion  
dc.date.updated
2022-07-04T19:59:05Z  
dc.journal.volume
27  
dc.journal.number
2  
dc.journal.pagination
1-13  
dc.journal.pais
Suiza  
dc.journal.ciudad
Basilea  
dc.description.fil
Fil: Larghi, Enrique Leandro. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; Argentina. Universite Paris-Saclay;  
dc.description.fil
Fil: Bruneau, Alexandre. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; Argentina  
dc.description.fil
Fil: Sauvage, Félix. Universite Paris-Saclay;  
dc.description.fil
Fil: Alami, Mouad. Universite Paris-Saclay;  
dc.description.fil
Fil: Vergnaud-Gauduchon, Juliette. Universite Paris-Saclay;  
dc.description.fil
Fil: Messaoudi, Samir. Universite Paris-Saclay;  
dc.journal.title
Molecules  
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/https://www.mdpi.com/1420-3049/27/2/412  
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.3390/molecules27020412