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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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| 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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