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dc.contributor.author
Dávila, Belén
dc.contributor.author
Sánchez, C.
dc.contributor.author
Fernandez, M.
dc.contributor.author
Cerecetto, H.
dc.contributor.author
Lecot, N.
dc.contributor.author
Cabral, P.
dc.contributor.author
Glisoni, Romina Julieta
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dc.contributor.author
González, M.
dc.date.available
2021-01-05T18:11:36Z
dc.date.issued
2019-08
dc.identifier.citation
Dávila, Belén; Sánchez, C.; Fernandez, M.; Cerecetto, H.; Lecot, N.; et al.; Selective Hypoxia-Cytotoxin 7-Fluoro-2-Aminophenazine 5,10-Dioxide: Toward Candidate-to-Drug Stage in the Drug-Development Pipeline; Wiley Blackwell Publishing, Inc; ChemistrySelect; 4; 32; 8-2019; 9396-9402
dc.identifier.issn
2365-6549
dc.identifier.uri
http://hdl.handle.net/11336/121516
dc.description.abstract
7-Fluoro-2-aminophenazine 5,10-dioxide, 1, has displayed in vitro bioreductive selective cytotoxicity, which could acts towards tumors containing hypoxic regions. In this work, we describe some preclinical studies of compound 1 confirming its in vivo antitumor activity. The synthesis of compound 1 was scaled up to 3 g improving the micro-scale yield. Some drug-like properties for compound 1 were theoretically-predicted and others, i.e. aqueous-solubility and toxicity -mutagenicity, in vivo chromosomal-aberrations and ip acute LD50-, were experimentally confirmed. Antitumoral activity was studied in mice bearing hypoxic 4T1-breast-tumor by assessing evolution of the tumor sizes, animal-survival and bio-chemical/hematological. Compound 1 in vivo efficacy, with the absence of systemic toxicity, was confirmed. Results highlight the potential of 7-fluoro-2-aminophenazine 5,10-dioxide as promissory therapeutic agentfor solid tumors.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
Wiley Blackwell Publishing, Inc
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dc.rights
info:eu-repo/semantics/restrictedAccess
dc.rights.uri
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.subject
PHENAZINE
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ANTITUMORAL CANDIDATE
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IN VIVO PROOF
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BREAST CANCER
dc.subject.classification
Química Orgánica
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dc.subject.classification
Ciencias Químicas
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CIENCIAS NATURALES Y EXACTAS
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dc.title
Selective Hypoxia-Cytotoxin 7-Fluoro-2-Aminophenazine 5,10-Dioxide: Toward Candidate-to-Drug Stage in the Drug-Development Pipeline
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2020-12-17T19:15:26Z
dc.journal.volume
4
dc.journal.number
32
dc.journal.pagination
9396-9402
dc.journal.pais
Alemania
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dc.description.fil
Fil: Dávila, Belén. Universidad de la República; Uruguay
dc.description.fil
Fil: Sánchez, C.. Universidad de la República; Uruguay
dc.description.fil
Fil: Fernandez, M.. Universidad de la República; Uruguay
dc.description.fil
Fil: Cerecetto, H.. Universidad de la República; Uruguay
dc.description.fil
Fil: Lecot, N.. Universidad de la República; Uruguay
dc.description.fil
Fil: Cabral, P.. Universidad de la República; Uruguay
dc.description.fil
Fil: Glisoni, Romina Julieta. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Nanobiotecnología. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Instituto de Nanobiotecnología; Argentina
dc.description.fil
Fil: González, M.. Universidad de la República; Uruguay
dc.journal.title
ChemistrySelect
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/https://onlinelibrary.wiley.com/doi/abs/10.1002/slct.201902601
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1002/slct.201902601
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