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dc.contributor.author
Acosta, Paola
dc.contributor.author
Butassi, Estefanía
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Insuasty, Braulio
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Ortiz, Alejandro
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Abonia, Rodrigo
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Zacchino, Susana Alicia Stella
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Quiroga, Jairo
dc.date.available
2022-12-05T19:42:49Z
dc.date.issued
2015-05
dc.identifier.citation
Acosta, Paola; Butassi, Estefanía; Insuasty, Braulio; Ortiz, Alejandro; Abonia, Rodrigo; et al.; Microwave-assisted synthesis of novel pyrazolo[3,4-g][1,8]naphthyridin-5-amine with potential antifungal and antitumor activity; Molecular Diversity Preservation International; Molecules; 20; 5; 5-2015; 8499-8520
dc.identifier.issn
1420-3049
dc.identifier.uri
http://hdl.handle.net/11336/180266
dc.description.abstract
The microwave assisted reaction between heterocyclic o-aminonitriles 1 and cyclic ketones 2 catalyzed by zinc chloride led to new series of pyrazolo[3,4-b] [1,8]naphthyridin-5-amines 3 in good yields. This procedure provides several advantages such as being environmentally friendly, high yields, simple work-up procedure, broad scope of applicability and the protocol provides an alternative for the synthesis of pyrazolonaphthyridines. The whole series showed antifungal activities against Candida albicans and Cryptococcus neoformans standardized strains, being compounds with a 4-p-tolyl substituent of the naphthyridin scheleton (3a, 3d and 3g), the most active ones mainly against C. albicans, which appear to be related to their comparative hydrophobicity. Among them, 3d, containing a cyclohexyl fused ring, showed the best activity. The anti-Candida activity was corroborated by testing the three most active compounds against clinical isolates of albicans and non-albicans Candida strains. These compounds were also screened by the US National Cancer Institute (NCI) for their ability to inhibit 60 different human tumor cell lines. Compounds 3a and 3e showed remarkable antitumor activity against cancer cell lines, with the most important GI50 values ranging from 0.62 to 2.18 μM.
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
ANTIFUNGAL ACTIVITY
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ANTITUMORAL ACTIVITY
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CANDIDA ALBICANS
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CRYPTOCOCCUS NEOFORMANS
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MICROWAVE IRRADIATION
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PYRAZOLONAPHTHYRIDINES
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Química Orgánica
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Ciencias Químicas
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CIENCIAS NATURALES Y EXACTAS
dc.title
Microwave-assisted synthesis of novel pyrazolo[3,4-g][1,8]naphthyridin-5-amine with potential antifungal and antitumor activity
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2022-12-05T15:06:17Z
dc.journal.volume
20
dc.journal.number
5
dc.journal.pagination
8499-8520
dc.journal.pais
Suiza
dc.journal.ciudad
Basel
dc.description.fil
Fil: Acosta, Paola. Universidad del Valle; Colombia
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Fil: Butassi, Estefanía. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Química Orgánica. Área Farmacognosia; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
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Fil: Insuasty, Braulio. Universidad del Valle; Colombia
dc.description.fil
Fil: Ortiz, Alejandro. Universidad del Valle; Colombia
dc.description.fil
Fil: Abonia, Rodrigo. Universidad del Valle; Colombia
dc.description.fil
Fil: Zacchino, Susana Alicia Stella. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Química Orgánica. Área Farmacognosia; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
dc.description.fil
Fil: Quiroga, Jairo. Universidad del Valle; Colombia
dc.journal.title
Molecules
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.3390/molecules20058499
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/https://www.mdpi.com/1420-3049/20/5/8499
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