2022-02-142022-02-142021-09-062046-2069http://hdl.handle.net/2133/23061The 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.application/pdf29741–29751engopenAccessCytotoxicityDrug productsCytotoxicHybrid compoundsOxadiazolespublishedVersionCamacho, Cristián MatíasPizzio, Marianela G.Roces, David L.Boggian, Dora BernardaMata, Ernesto GabinoBellizzi, YaninaBarrionuevo, ElizabethBlank, Viviana C.Roguin, Leonor P.Atribución-NoComercial 3.0 Unported (CC BY-NC 3.0)