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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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| Araújo,Flávio Henrique Souza de; Figueiredo,Débora Rojas de; Auharek,Sarah Alves; Pesarini,João Renato; Meza,Alisson; Gomes,Roberto da Silva; Monreal,Antônio Carlos Duenhas; Antoniolli-Silva,Andréia Conceição Milan Brochado; Lima,Dênis Pires de; Kassuya,Candida Aparecida Leite; Beatriz,Adilson; Oliveira,Rodrigo Juliano. |
| Abstract Chemotherapy is one of the major approaches for the treatment of cancer. Therefore, the development of new chemotherapy drugs is an important aspect of medicinal chemistry. Chemotherapeutic agents include isocoumarins, which are privileged structures with potential antitumoral activity. Herein, a new 3-substituted isocoumarin was synthesized from 2-iodo-3,5-dimethoxy-benzoic acid and oct-1-yne in a cross-coupling Sonogashira reaction followed by a copper iodide-catalyzed intramolecular cyclization as key step using MeOH/Et3N as the solvent system. The present study also evaluated the leukometry, phagocytic activity, genotoxic potential and cell death induction of three different doses (5 mg/kg, 10 mg/kg and 20 mg/kg) of this newly synthesized... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Isocoumarin synthesis; Genotoxicity; Splenic phagocytosis; Chemotherapy. |
| Ano: 2017 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1415-47572017000400665 |
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