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| Juliano Oliveira,Rodrigo; Pereira,Fabrícia Paniago Ajala Nery; Silveira,Ingridhy Ostaciana Maia Freitas da; Lima,Ricardo Vieira de; Berno,Claudia Rodrigues; Pesarini,João Renato; Antoniolli-Silva,Andréia Conceição Milan Brochado; Monreal,Antônio Carlos Duenhas; Adilson,Beatriz; Lima,Dênis Pires de; Gomes,Roberto da Silva. |
| Abstract Despite rapid advances in both the early detection and treatment of cancer, the mortality from this disease remains high, which justifies the development of new products that are more selective and effective and have fewer side effects. Accordingly, a novel ester was synthesized that contains two pharmacophores with important biological activities: (I) 4-aminoantipyrine, which has anti-inflammatory and antioxidant effects, and (II) the pharmacophore 1,4-dioxo-butenyl, which has cytotoxic activity. When administered alone, this compound is non-genotoxic, and it does not cause an increasing in splenic phagocytosis. Nevertheless, it can induce cell death. When administered in combination with commercial chemotherapeutic agents, such as doxorubicin,... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Cancer 4-aminoantipyrine 1; 4-dioxo-butenyl chemoprevention chemotherapy. |
| Ano: 2019 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1415-47572019000300399 |
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| Oliveira,Rodrigo Juliano; da Cruz Leite Santos,Naiara; Pesarini,João Renato; de Oliveira,Beatriz Carneiro; Berno,Claudia Rodrigues; de Araújo,Flávio Henrique Souza; da Silveira,Ingridhy Ostaciana Maia Freitas; Nascimento,Raquel Oliveira; Brochado Antoniolli-Silva,Andréia Conceição Milan; Duenhas Monreal,Antônio Carlos; Beatriz,Adilson; de Lima,Dênis Pires; da Silva Gomes,Roberto. |
| Abstract The increased incidence of cancer and its high treatment costs have encouraged the search for new compounds to be used in adjuvant therapies for this disease. This study discloses the synthesis of (Z)-4-((1,5-dimethyl-3-oxo-2-phenyl-2,3dihydro-1H-pyrazol-4-yl) amino)-4-oxobut-2-enoic acid (IR-01) and evaluates not only the action of this compound on genetic integrity, increase in splenic phagocytosis and induction of cell death but also its effects in combination with the commercial chemotherapeutic agents doxorubicin, cisplatin and cyclophosphamide. IR-01 was designed and synthesized based on two multifunctionalyzed structural fragments: 4-aminoantipyrine, an active dipyrone metabolite, described as an antioxidant and anti-inflammatory agent; and... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Splenic phagocytosis; Comet assay; Micronucleus test; Cell death; Chemoprevention. |
| Ano: 2018 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1415-47572018000100154 |
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