Por favor, use este identificador para citar o enlazar a este item:
http://hdl.handle.net/10261/213190
COMPARTIR / EXPORTAR:
SHARE CORE BASE | |
Visualizar otros formatos: MARC | Dublin Core | RDF | ORE | MODS | METS | DIDL | DATACITE | |
Título: | Synthesis and biological evaluation of crown ether acyl derivatives |
Autor: | Febles, M. CSIC ORCID; Montalvão, Sofía; Díaz Crespín, Guillermo; Norte, Manuel; Padrón, José M.; Tammela, Päivi; Fernández, José J.; Hernández Daranas, Antonio CSIC ORCID | Palabras clave: | Crown ether Antiproliferative Antimicrobial Structure–activity 18-Crown-6 |
Fecha de publicación: | 15-nov-2016 | Editor: | Elsevier | Citación: | Bioorganic and Medicinal Chemistry Letters 26(22): 5591-5593 (2016) | Resumen: | A set of crown ethyl acyl derivatives based on 18-crown-6 moiety was synthesized and evaluated for biological activity. In vitro antiproliferative profiling demonstrated significant activities against HBL-100, HeLa, SW1573 and WiDr human cell lines. The most active compound exhibited GI50 values in the range of 3.7–5.6 μM. Antimicrobial evaluation showed that three polyaromatic compounds were active against Staphylococcus aureus (MIC90 values from 8.3 μM to 50 μM), whereas a (decyloxy)benzene substitution exhibited moderate activity against Candida albicans (MIC90 values 36 μM). According to SAR evaluation, the size of the crown ether and the acyl side chain had a significant effect on the bioactivity. Aromatic moieties close to the acyl group led to improved bioactivity as exemplified by some of the tested compounds. These results provide further evidence on the potential of crown ethyl structure as a scaffold for developing new biological probes and lead candidates for drug development. | Versión del editor: | https://doi.org/10.1016/j.bmcl.2016.09.066 | URI: | http://hdl.handle.net/10261/213190 | DOI: | 10.1016/j.bmcl.2016.09.066 | ISSN: | 0960-894X | E-ISSN: | 1464-3405 |
Aparece en las colecciones: | (IPNA) Artículos |
Ficheros en este ítem:
Fichero | Descripción | Tamaño | Formato | |
---|---|---|---|---|
accesoRestringido.pdf | Artículo principal | 16,34 kB | Adobe PDF | Visualizar/Abrir |
CORE Recommender
SCOPUSTM
Citations
14
checked on 11-abr-2024
WEB OF SCIENCETM
Citations
13
checked on 28-feb-2024
Page view(s)
111
checked on 19-abr-2024
Download(s)
21
checked on 19-abr-2024
Google ScholarTM
Check
Altmetric
Altmetric
Este item está licenciado bajo una Licencia Creative Commons