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dc.contributor.author
Moreno, Leydi M.
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Quiroga, Jairo
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Abonia, Rodrigo
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Crespo, María del P.
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Aranaga, Carlos
dc.contributor.author
Martínez Martínez, Luis
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Sortino, Maximiliano Andrés
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Barreto, Mauricio
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Burbano, María E.
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Insuasty, Braulio
dc.date.available
2024-04-19T14:18:51Z
dc.date.issued
2024-03
dc.identifier.citation
Moreno, Leydi M.; Quiroga, Jairo; Abonia, Rodrigo; Crespo, María del P.; Aranaga, Carlos; et al.; Synthesis of Novel Triazine-Based Chalcones and 8,9-dihydro-7H-pyrimido[4,5-b][1,4]diazepines as Potential Leads in the Search of Anticancer, Antibacterial and Antifungal Agents; Molecular Diversity Preservation International; International Journal of Molecular Sciences; 25; 7; 3-2024; 1-24
dc.identifier.issn
1422-0067
dc.identifier.uri
http://hdl.handle.net/11336/233592
dc.description.abstract
This study presents the synthesis of four series of novel hybrid chalcones (20,21)a–g and (23,24)a–g and six series of 1,3,5-triazine-based pyrimido[4,5-b][1,4]diazepines (28–33)a–g and the evaluation of their anticancer, antibacterial, antifungal, and cytotoxic properties. Chalcones 20b,d, 21a,b,d, 23a,d–g, 24a–g and the pyrimido[4,5-b][1,4]diazepines 29e,g, 30g, 31a,b,e–g, 33a,b,e–g exhibited outstanding anticancer activity against a panel of 60 cancer cell lines with GI50 values between 0.01 and 100 μM and LC50 values in the range of 4.09 μM to >100 μM, several of such derivatives showing higher activity than the standard drug 5-fluorouracil (5-FU). On the other hand, among the synthesized compounds, the best antibacterial properties against N. gonorrhoeae, S. aureus (ATCC 43300), and M. tuberculosis were exhibited by the pyrimido[4,5-b][1,4]diazepines (MICs: 0.25–62.5 µg/mL). The antifungal activity studies showed that triazinylamino-chalcone 29e and triazinyloxy-chalcone 31g were the most active compounds against T. rubrum and T. mentagrophytes and A. fumigatus, respectively (MICs = 62.5 μg/mL). Hemolytic activity studies and in silico toxicity analysis demonstrated that most of the compounds are safe.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
Molecular Diversity Preservation International
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dc.rights
info:eu-repo/semantics/openAccess
dc.rights.uri
https://creativecommons.org/licenses/by/2.5/ar/
dc.subject
1,3,5-TRIAZINES
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CHALCONES
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DIAZEPINES
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ANTICANCER ACTIVITY
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ANTIBACTERIAL ACTIVITY
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ANTIFUNGAL ACTIVITY
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CYTOTOXICITY
dc.subject.classification
Química Orgánica
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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 Triazine-Based Chalcones and 8,9-dihydro-7H-pyrimido[4,5-b][1,4]diazepines as Potential Leads in the Search of Anticancer, Antibacterial and Antifungal 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
2024-04-12T13:04:18Z
dc.journal.volume
25
dc.journal.number
7
dc.journal.pagination
1-24
dc.journal.pais
Suiza
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dc.journal.ciudad
Basilea
dc.description.fil
Fil: Moreno, Leydi M.. Universidad del Valle; 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: Crespo, María del P.. Universidad del Valle; Colombia
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Fil: Aranaga, Carlos. Universidad de Santiago de Cali; Colombia. Universidad de Córdoba; España
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Fil: Martínez Martínez, Luis. Universidad de Córdoba; España
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Fil: Sortino, Maximiliano Andrés. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario; Argentina. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Química Orgánica. Área Farmacognosia; Argentina
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Fil: Barreto, Mauricio. Universidad del Valle; Colombia
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Fil: Burbano, María E.. Universidad del Valle; Colombia
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Fil: Insuasty, Braulio. Grupo de Investigación de Compuestos Heterocíclicos; Colombia
dc.journal.title
International Journal of Molecular Sciences
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dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/https://www.mdpi.com/1422-0067/25/7/3623
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.3390/ijms25073623
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