Design, synthesis and cytotoxic evaluation of a library of oxadiazole-containing hybrids
The development of hybrid compounds led to the discovery of new pharmacologically active agents for some of the most critical diseases, including cancer. Herein, we describe a new series of oxadiazole-containing structures designed by a molecular hybridization approach. Penicillin derivatives and am...
| Autores principales: | , , , , , , , , |
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| Formato: | article artículo publishedVersion |
| Lenguaje: | Inglés |
| Publicado: |
Royal Society of Chemistry
2022
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| Materias: | |
| Acceso en línea: | http://hdl.handle.net/2133/23061 http://hdl.handle.net/2133/23061 |
| Aporte de: |
| id |
I15-R121-2133-23061 |
|---|---|
| record_format |
dspace |
| institution |
Universidad Nacional de Rosario |
| institution_str |
I-15 |
| repository_str |
R-121 |
| collection |
Repositorio Hipermedial de la Universidad Nacional de Rosario (UNR) |
| language |
Inglés |
| orig_language_str_mv |
eng |
| topic |
Cytotoxicity Drug products Cytotoxic Hybrid compounds Oxadiazoles |
| spellingShingle |
Cytotoxicity Drug products Cytotoxic Hybrid compounds Oxadiazoles Camacho, Cristián Matías Pizzio, Marianela G. Roces, David L. Boggian, Dora Bernarda Mata, Ernesto Gabino Bellizzi, Yanina Barrionuevo, Elizabeth Blank, Viviana C. Roguin, Leonor P. Design, synthesis and cytotoxic evaluation of a library of oxadiazole-containing hybrids |
| topic_facet |
Cytotoxicity Drug products Cytotoxic Hybrid compounds Oxadiazoles |
| description |
The development of hybrid compounds led to the discovery of new pharmacologically active agents for some of the most critical diseases, including cancer. Herein, we describe a new series of oxadiazole-containing structures designed by a molecular hybridization approach. Penicillin derivatives and amino acids were linked to amino acid and aromatic moieties through the formation of a 1,2,4-oxadiazole ring. Alternatively, condensation between amino acid-derived hydrazides and an activated penicillanic acid led to a series of 1,3,4-oxadiazole penicillin-containing hybrids and non-cyclized diacylhydrazides. From the cytotoxicity assays it is highlighted that two 1,2,4-oxadiazoles and one 1,3,4-oxadiazole connecting a penicillin and aliphatic amino acids displayed a high degree of cytotoxic selectivity, ranging between being three and four times more potent against tumor cells than normal cells. The results give a very interesting perspective suggesting that these hybrid compounds can offer a novel antitumor scaffold with promising cytotoxicity profiles. |
| format |
article artículo publishedVersion |
| author |
Camacho, Cristián Matías Pizzio, Marianela G. Roces, David L. Boggian, Dora Bernarda Mata, Ernesto Gabino Bellizzi, Yanina Barrionuevo, Elizabeth Blank, Viviana C. Roguin, Leonor P. |
| author_facet |
Camacho, Cristián Matías Pizzio, Marianela G. Roces, David L. Boggian, Dora Bernarda Mata, Ernesto Gabino Bellizzi, Yanina Barrionuevo, Elizabeth Blank, Viviana C. Roguin, Leonor P. |
| author_sort |
Camacho, Cristián Matías |
| title |
Design, synthesis and cytotoxic evaluation of a library of oxadiazole-containing hybrids |
| title_short |
Design, synthesis and cytotoxic evaluation of a library of oxadiazole-containing hybrids |
| title_full |
Design, synthesis and cytotoxic evaluation of a library of oxadiazole-containing hybrids |
| title_fullStr |
Design, synthesis and cytotoxic evaluation of a library of oxadiazole-containing hybrids |
| title_full_unstemmed |
Design, synthesis and cytotoxic evaluation of a library of oxadiazole-containing hybrids |
| title_sort |
design, synthesis and cytotoxic evaluation of a library of oxadiazole-containing hybrids |
| publisher |
Royal Society of Chemistry |
| publishDate |
2022 |
| url |
http://hdl.handle.net/2133/23061 http://hdl.handle.net/2133/23061 |
| work_keys_str_mv |
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Repositorios |
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