Design, synthesis and cytotoxic evaluation of a library of oxadiazole-containing hybrids

dc.creatorCamacho, Cristián Matías
dc.creatorPizzio, Marianela G.
dc.creatorRoces, David L.
dc.creatorBoggian, Dora Bernarda
dc.creatorMata, Ernesto Gabino
dc.creatorBellizzi, Yanina
dc.creatorBarrionuevo, Elizabeth
dc.creatorBlank, Viviana C.
dc.creatorRoguin, Leonor P.
dc.date2022-02-14T18:56:12Z
dc.date2022-02-14T18:56:12Z
dc.date2021-09-06
dc.date2022-02-14T18:56:12Z
dc.date2022-02-14T18:56:12Z
dc.date2021-09-06
dc.identifier2046-2069
dc.identifierhttp://hdl.handle.net/2133/23061
dc.identifierhttp://hdl.handle.net/2133/23061
dc.descriptionThe 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.
dc.descriptionFil: Camacho, Cristián Matías. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario (CONICET-UNR); Argentina.
dc.descriptionFil: Pizzio, Marianela G. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario (CONICET-UNR); Argentina.
dc.descriptionFil: Roces, David L. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario (CONICET-UNR); Argentina.
dc.descriptionFil: Boggian, Dora Bernarda. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario (CONICET-UNR); Argentina.
dc.descriptionFil: Mata, Ernesto Gabino. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario (CONICET-UNR); Argentina.
dc.descriptionFil: Bellizzi, Yanina. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Instituto de Química y Fisicoquímica Biológicas (UBA–CONICET); Argentina.
dc.descriptionFil: Blank, Viviana C. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Instituto de Química y Fisicoquímica Biológicas (UBA–CONICET); Argentina.
dc.descriptionFil: Roguin, Leonor P. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Instituto de Química y Fisicoquímica Biológicas (UBA–CONICET); Argentina.
dc.formatapplication/pdf
dc.languageeng
dc.publisherRoyal Society of Chemistry
dc.relationhttps://pubs.rsc.org/en/content/articlelanding/2021/RA/d1ra05602f
dc.relationhttps://doi.org/10.1039/D1RA05602F
dc.rightshttps://creativecommons.org/licenses/by-nc/3.0/
dc.rightsCamacho, Cristián Matías
dc.rightsPizzio, Marianela G.
dc.rightsRoces, David L.
dc.rightsBoggian, Dora Bernarda
dc.rightsMata, Ernesto Gabino
dc.rightsBellizzi, Yanina
dc.rightsBarrionuevo, Elizabeth
dc.rightsBlank, Viviana C.
dc.rightsRoguin, Leonor P.
dc.rightsAtribución-NoComercial 3.0 Unported (CC BY-NC 3.0)
dc.rightsopenAccess
dc.subjectCytotoxicity
dc.subjectDrug products
dc.subjectCytotoxic
dc.subjectHybrid compounds
dc.subjectOxadiazoles
dc.titleDesign, synthesis and cytotoxic evaluation of a library of oxadiazole-containing hybrids
dc.typepublishedVersion
dc.typearticle
dc.typeartículo


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