Registro completo de metadatos
| Campo DC | Valor | Lengua/Idioma |
|---|---|---|
| dc.creator | Ramírez, Juan | - |
| dc.creator | Svetaz, Laura Andrea | - |
| dc.creator | Quiroga, Jairo | - |
| dc.creator | Abonia, Rodrigo | - |
| dc.creator | Raimondi, Marcela | - |
| dc.creator | Zacchino, Susana | - |
| dc.creator | Insuasty, Braulio | - |
| dc.date | 2017-02-24T14:24:00Z | - |
| dc.date | 2017-02-24T14:24:00Z | - |
| dc.date | 2015-03 | - |
| dc.date | 2017-02-23T13:56:21Z | - |
| dc.date.accessioned | 2019-04-29T15:45:33Z | - |
| dc.date.available | 2019-04-29T15:45:33Z | - |
| dc.date.issued | 2015-03 | - |
| dc.identifier | Ramírez, Juan; Svetaz, Laura Andrea; Quiroga, Jairo; Abonia, Rodrigo; Raimondi, Marcela; et al.; Synthesis of novel thiazole-based 8,9-dihydro-7H-pyrimido[4,5-b][1,4]diazepines as potential antitumor and antifungal agents; Elsevier Masson; European Journal Of Medical Chemistry; 92; 3-2015; 866–875 | - |
| dc.identifier | 0223-5234 | - |
| dc.identifier | http://hdl.handle.net/11336/13358 | - |
| dc.identifier.uri | http://rodna.bn.gov.ar:8080/jspui/handle/bnmm/301308 | - |
| dc.description | A new series of novel thiazole-based 8,9-dihydro-7H-pyrimido[4,5-b][1,4]diazepines 6a–g and 7a–g were obtained with high regioselectivity from the reaction of triamino- or tetraaminopyrimidines 4 and 5 with α,β-unsaturated carbonyl compounds 3a–g based on 2,4-dichlorothiazol-5-carbaldehyde 1. Twelve of the synthesized compounds were selected and tested by US National Cancer Institute (NCI) for their antitumor activity against 60 different human tumor cell lines. Compounds 7d and 7g showed important GI50 ranges of 1.28–2.98 μM and 0.35–2.78 μM respectively under in vitro assays. In addition, 6a–g and 7a–g were tested for antifungal properties against the clinical important fungi Candida albicans and Cryptococcus neoformans. Although these compounds showed moderate activities against C. albicans, the 2-amino derivatives 7a–g and mainly 7a and 7b, showed high activity against standardized and clinical isolates of C. neoformans with MIC50 = 7.8–31.2 μg/mL, MIC80 = 15.6–31.2 μg/mL and MIC100 = 15.6–62.5 μg/mL. In addition, since both compounds were fungicide rather than fungistatic these thiazole-based 8,9-dihydro-7H-pyrimido[4,5-b][1,4]diazepines appear as good candidates for further development not only as antifungal but also as antitumor drugs. | - |
| dc.description | Fil: Ramírez, Juan. Universidad del Valle. Departamento de Química; Colombia | - |
| dc.description | Fil: Svetaz, Laura Andrea. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Cientifico Tecnológico Rosario; Argentina. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Química Orgánica. Area Farmacognosia; Argentina | - |
| dc.description | Fil: Quiroga, Jairo. Universidad del Valle. Departamento de Química; Colombia | - |
| dc.description | Fil: Abonia, Rodrigo. Universidad del Valle. Departamento de Química; Colombia | - |
| dc.description | Fil: Raimondi, Marcela. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Química Orgánica. Area Farmacognosia; Argentina | - |
| dc.description | Fil: Zacchino, Susana. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Química Orgánica. Area Farmacognosia; Argentina | - |
| dc.description | Fil: Insuasty, Braulio. Universidad del Valle. Departamento de Química; Colombia | - |
| dc.format | application/pdf | - |
| dc.format | application/pdf | - |
| dc.format | application/pdf | - |
| dc.language | eng | - |
| dc.publisher | Elsevier Masson | - |
| dc.relation | info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1016/j.ejmech.2015.01.053 | - |
| dc.relation | info:eu-repo/semantics/altIdentifier/url/http://www.sciencedirect.com/science/article/pii/S0223523415000732 | - |
| dc.rights | info:eu-repo/semantics/restrictedAccess | - |
| dc.rights | https://creativecommons.org/licenses/by-nc-sa/2.5/ar/ | - |
| dc.source | reponame:CONICET Digital (CONICET) | - |
| dc.source | instname:Consejo Nacional de Investigaciones Científicas y Técnicas | - |
| dc.source | instacron:CONICET | - |
| dc.subject | Thiazole | - |
| dc.subject | Regioselectivity | - |
| dc.subject | Pyrimido[4,5-b][1,4]diazepines | - |
| dc.subject | Antitumor activity | - |
| dc.subject | Antifungal activity | - |
| dc.subject | Química Orgánica | - |
| dc.subject | Ciencias Químicas | - |
| dc.subject | CIENCIAS NATURALES Y EXACTAS | - |
| dc.title | Synthesis of novel thiazole-based 8,9-dihydro-7H-pyrimido[4,5-b][1,4]diazepines as potential antitumor and antifungal agents | - |
| dc.type | info:eu-repo/semantics/article | - |
| dc.type | info:eu-repo/semantics/publishedVersion | - |
| dc.type | info:ar-repo/semantics/articulo | - |
| Aparece en las colecciones: | CONICET | |
Ficheros en este ítem:
No hay ficheros asociados a este ítem.