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dc.contributor.author
Malvacio, Ivana
dc.contributor.author
Cuzzolin, Alberto
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Sturlese, Mattia
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Vera, Domingo Mariano Adolfo
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Moyano, Elizabeth Laura
dc.contributor.author
Moro, Stefano
dc.date.available
2018-05-02T18:42:15Z
dc.date.issued
2017-12
dc.identifier.citation
Malvacio, Ivana; Cuzzolin, Alberto; Sturlese, Mattia; Vera, Domingo Mariano Adolfo; Moyano, Elizabeth Laura; et al.; Synthesis and preliminary structure-activity relationship study of 2-aryl-2 H -pyrazolo[4,3- c ]quinolin-3-ones as potential checkpoint kinase 1 (Chk1) inhibitors; Taylor & Francis Ltd; Journal of Enzyme Inhibition and Medicinal Chemistry; 33; 1; 12-2017; 171-183
dc.identifier.issn
1475-6366
dc.identifier.uri
http://hdl.handle.net/11336/43913
dc.description.abstract
The serine-threonine checkpoint kinase 1 (Chk1) plays a critical role in the cell cycle arrest in response to DNA damage. In the last decade, Chk1 inhibitors have emerged as a novel therapeutic strategy to potentiate the anti-tumour efficacy of cytotoxic chemotherapeutic agents. In the search for new Chk1 inhibitors, a congeneric series of 2-aryl-2 H-pyrazolo[4,3-c]quinolin-3-one (PQ) was evaluated by in-vitro and in-silico approaches for the first time. A total of 30 PQ structures were synthesised in good to excellent yields using conventional or microwave heating, highlighting that 14 of them are new chemical entities. Noteworthy, in this preliminary study two compounds 4e 2 and 4h 2 have shown a modest but significant reduction in the basal activity of the Chk1 kinase. Starting from these preliminary results, we have designed the second generation of analogous in this class and further studies are in progress in our laboratories.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
Taylor & Francis Ltd
dc.rights
info:eu-repo/semantics/openAccess
dc.rights.uri
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.subject
2-Aryl-2h-Pyrazolo[4,3-C]Qui- Nolin-3-One
dc.subject
Serine- Threonine Checkpoint Kinase 1 (Chk1)
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Molecular Docking
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Molecular Dynamics
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Otras Ciencias Químicas
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Ciencias Químicas
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CIENCIAS NATURALES Y EXACTAS
dc.title
Synthesis and preliminary structure-activity relationship study of 2-aryl-2 H -pyrazolo[4,3- c ]quinolin-3-ones as potential checkpoint kinase 1 (Chk1) inhibitors
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2018-04-16T14:42:04Z
dc.journal.volume
33
dc.journal.number
1
dc.journal.pagination
171-183
dc.journal.pais
Reino Unido
dc.journal.ciudad
Londres
dc.description.fil
Fil: Malvacio, Ivana. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Investigaciones en Físico-química de Córdoba. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Instituto de Investigaciones en Físico-química de Córdoba; Argentina
dc.description.fil
Fil: Cuzzolin, Alberto. Università di Padova; Italia
dc.description.fil
Fil: Sturlese, Mattia. Università di Padova; Italia
dc.description.fil
Fil: Vera, Domingo Mariano Adolfo. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Mar del Plata. Instituto de Investigaciones en Biodiversidad y Biotecnología; Argentina
dc.description.fil
Fil: Moyano, Elizabeth Laura. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Investigaciones en Físico-química de Córdoba. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Instituto de Investigaciones en Físico-química de Córdoba; Argentina
dc.description.fil
Fil: Moro, Stefano. Università di Padova; Italia
dc.journal.title
Journal of Enzyme Inhibition and Medicinal Chemistry
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1080/14756366.2017.1404592
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/https://www.tandfonline.com/doi/full/10.1080/14756366.2017.1404592
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