Full metadata record
DC Field | Value | Language |
---|---|---|
dc.creator | Gonda, M. (Mariana) | - |
dc.creator | Nieves, M. (Marcos) | - |
dc.creator | Nunes, E. (Elia) | - |
dc.creator | Lopez-de-Cerain, A. (Adela) | - |
dc.creator | Monge, A. (Antonio) | - |
dc.creator | Lavaggi, M.L. (María L.) | - |
dc.creator | Gonzalez, M. (Mercedes) | - |
dc.creator | Cerecetto, H. (Hugo) | - |
dc.date.accessioned | 2014-11-14T13:50:44Z | - |
dc.date.available | 2014-11-14T13:50:44Z | - |
dc.date.issued | 2013 | - |
dc.identifier.citation | Gonda M, Nieves M, Nunes E, López-de-Ceráin A, Monge A, Lavaggi ML, et al. Phenazine N,N′-dioxide scaffold as selective hypoxic cytotoxin pharmacophore. Structural modifications looking for further DNA topoisomerase II-inhibition activity. Med Chem Commun. 2013;4:595-607 | es_ES |
dc.identifier.issn | 2040-2503 | - |
dc.identifier.uri | https://hdl.handle.net/10171/37046 | - |
dc.description.abstract | Phenazine-5,10-dioxides have been identified as prodrugs for antitumour therapy that undergo hypoxic-selective bioreduction, in the solid tumour cells, to form cytotoxic species. We investigated structural modifications of the phenazine-5,10-dioxide scaffold attempting to find new selective hypoxic cytotoxins with additional ability to inhibit DNA topoisomerase II. Four series of new phenazine-5,10-dioxides aryl-substituted connected by different linkers were prepared. The clonogenic survivals of V79 cells on aerobic and anaerobic conditions were determined, and studies of oxic DNA-interaction and hypoxic DNA topoisomerase II-inhibition, for the most relevant derivatives, were performed. Four new hypoxic-selective cytotoxins were identified at the assayed doses. In some of them were operative the DNA-interaction and/or the inhibition of DNA topoisomerase II. For one of the unselective cytotoxin biotransformation studies were performed on aerobic and anaerobic conditions, explaining the lack of selectivity. | es_ES |
dc.language.iso | eng | es_ES |
dc.publisher | Royal Society of Chemistry | es_ES |
dc.rights | info:eu-repo/semantics/openAccess | es_ES |
dc.subject | Phenazine | es_ES |
dc.subject | DNA | es_ES |
dc.subject | Structure | es_ES |
dc.title | Phenazine N,N′-dioxide scaffold as selective hypoxic cytotoxin pharmacophore. Structural modifications looking for further DNA topoisomerase II-inhibition activity | es_ES |
dc.type | info:eu-repo/semantics/article | es_ES |
dc.identifier.doi | http://dx.doi.org/10.1039/C3MD00022B | es_ES |
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