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dc.contributor.author
Ramirez Prada, Jonathan
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Robledo, Sara M.
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Velez, Ivan D.
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Crespo, Maria del Pilar
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Quiroga, Jairo
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Abonia, Rodrigo
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Montoya, Alba
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Svetaz, Laura Andrea
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Zacchino, Susana Alicia Stella
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Insuasty, Braulio
dc.date.available
2018-07-26T14:53:08Z
dc.date.issued
2017-03
dc.identifier.citation
Ramirez Prada, Jonathan; Robledo, Sara M.; Velez, Ivan D.; Crespo, Maria del Pilar; Quiroga, Jairo; et al.; Synthesis of novel quinoline–based 4,5–dihydro–1H–pyrazoles as potential anticancer, antifungal, antibacterial and antiprotozoal agents; Elsevier France-editions Scientifiques Medicales Elsevier; European Journal of Medical Chemistry; 131; 3-2017; 237-254
dc.identifier.issn
0223-5234
dc.identifier.uri
http://hdl.handle.net/11336/53154
dc.description.abstract
A new series of N–substituted 2–pyrazolines 9a–f, 10a–f, 11a–f, 12a–f and 13a–f were obtained from the cyclocondensation reaction of [(7–chloroquinolin–4–yl)amino]chalcones 8a–f with hydrazine hydrate and its derivatives. Fourteen of the synthesized compounds including the starting chalcones were selected by US National Cancer Institute (NCI) for testing their anticancer activity against 60 different human cancer cell lines, with the most important GI50 values ranging from 0.28 to 11.7 μM (0.13–6.05 μg/mL) and LC50 values ranging from 2.6 to > 100 μM (1.2 to > 51.7 μg/mL), for chalcones 8a,d and pyrazolines 10c,d. All compounds were assessed for antibacterial activity against wild type and multidrug resistant gram negative and gram positive bacteria, with MIC values ranging from 31.25 to 500 μg/mL. Additionally, the novel compounds were tested for antifungal and antiparasitic properties. Although these compounds showed mild activity against Candida albicans, chalcones 8a and 8e showed high activity against Cryptococcus neoformans with MIC50 = 7.8 μg/mL. For anti–Plasmodium falciparum activity the 2–pyrazoline 11b was the most active with EC50 = 5.54 μg/mL. Regarding the activity against Trypanosoma cruzi, compound 10a was highly active with EC50 = 0.70 μg/mL. Chalcone 8a had good activity against Leishmania panamensis amastigotes with EC50 = 0.79 μg/mL.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
Elsevier France-editions Scientifiques Medicales Elsevier
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dc.rights
info:eu-repo/semantics/openAccess
dc.rights.uri
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.subject
2&Ndash;Pyrazolines
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Antibacterial Activity
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Anticancer Activity
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Antifungal Activity
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Antileishmanial Activity
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Antimalarial Activity
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Antitrypanosomal Activity
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Chalcones
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Quinoline
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Otras Ciencias Químicas
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dc.subject.classification
Ciencias Químicas
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CIENCIAS NATURALES Y EXACTAS
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dc.title
Synthesis of novel quinoline–based 4,5–dihydro–1H–pyrazoles as potential anticancer, antifungal, antibacterial and antiprotozoal agents
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2018-07-26T13:57:17Z
dc.journal.volume
131
dc.journal.pagination
237-254
dc.journal.pais
Francia
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dc.journal.ciudad
Paris
dc.description.fil
Fil: Ramirez Prada, Jonathan. Universidad del Valle; Colombia
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Fil: Robledo, Sara M.. Universidad de Antioquia; Chile
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Fil: Velez, Ivan D.. Universidad de Antioquia; Chile
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Fil: Crespo, Maria del Pilar. Universidad del Valle; Colombia. Universidad Santiago de Cali; Colombia
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Fil: Quiroga, Jairo. Universidad del Valle; Colombia
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Fil: Abonia, Rodrigo. Universidad del Valle; Colombia
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Fil: Montoya, Alba. Universidad del Valle; Colombia
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Fil: Svetaz, Laura Andrea. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Química Orgánica. Área Farmacognosia; Argentina
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Fil: Zacchino, Susana Alicia Stella. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Química Orgánica. Área Farmacognosia; Argentina
dc.description.fil
Fil: Insuasty, Braulio. Universidad del Valle; Colombia
dc.journal.title
European Journal of Medical Chemistry
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dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/https://dx.doi.org/10.1016/j.ejmech.2017.03.016
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/https://www.sciencedirect.com/science/article/pii/S0223523417301733
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