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Anticancer potential of benzothiazolic derivative (E)-2-((2-(benzo[d]thiazol-2-yl)hydrazono)methyl)-4-nitrophenol against melanoma cells.
Vasconcelos, Zanair Soares; Ralph, Ana Carolina Lima; Calcagno, Danielle Queiroz; Dos Santos Barbosa, Gleyce; do Nascimento Pedrosa, Tatiana; Antony, Lucas Pio; de Arruda Cardoso Smith, Marília; de Lucas Chazin, Eliza; Vasconcelos, Thatyana Rocha Alves; Montenegro, Raquel Carvalho; de Vasconcellos, Marne Carvalho.
Affiliation
  • Vasconcelos ZS; Faculty of Pharmaceutical Sciences, Federal University of Amazon, Amazon, Brazil.
  • Ralph ACL; Faculty of Pharmaceutical Sciences, Federal University of Amazon, Amazon, Brazil.
  • Calcagno DQ; Center on Oncology Research, Federal University of Pará, Pará, Brazil.
  • Dos Santos Barbosa G; Faculty of Pharmaceutical Sciences, Federal University of Amazon, Amazon, Brazil.
  • do Nascimento Pedrosa T; Faculty of Pharmaceutical Sciences, Federal University of Amazon, Amazon, Brazil.
  • Antony LP; Faculty of Pharmaceutical Sciences, Federal University of Amazon, Amazon, Brazil.
  • de Arruda Cardoso Smith M; Department of Morphology and Genetics, Paulista School of Medicine, Federal University of São Paulo, São Paulo, Brazil.
  • de Lucas Chazin E; Chemistry Institute, Fluminense Federal University, Rio de Janeiro, Brazil.
  • Vasconcelos TRA; Chemistry Institute, Fluminense Federal University, Rio de Janeiro, Brazil.
  • Montenegro RC; Drug Research and Development Center, Faculty of Medicine, Federal University of Ceará, Ceará, Brazil.
  • de Vasconcellos MC; Faculty of Pharmaceutical Sciences, Federal University of Amazon, Amazon, Brazil. Electronic address: marne@ufam.edu.br.
Toxicol In Vitro ; 50: 225-235, 2018 Aug.
Article in En | MEDLINE | ID: mdl-29574239
ABSTRACT
Malignant melanoma is an important type of cancer worldwide due to its aggressiveness and poor survival rate. Significant efforts to understand the biology of melanoma and approaches to treat the advanced disease are focused on targeted gene inhibitors. Frequently mutated genes, such as NRAS, B-RAF and TP53, significantly exceed the frequency of mutations of other genes, emphasizing their importance for future targeted therapies. Considering the antitumor activity of benzothiazolic derivatives, this study aimed to demonstrate the action of benzothiazolic (E)-2-((2-(benzo[d]thiazol-2-yl)hydrazono)methyl)-4-nitrophenol (AFN01) against three established human melanoma cell lines that recapitulate the molecular landscape of the disease in terms of its genetic alterations and mutations, such as the TP53, NRAS and B-RAF genes. The results presented here indicate that AFN01, as a significant cytostatic and cytotoxic drug due to its induction of DNA fragmentation, causes single and double DNA strand breaks, consequently inhibiting cell proliferation, migration and invasion by promoting apoptosis. Our data suggest that AFN01 might be considered as a future therapeutic option for managing melanoma.
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Full text: 1 Database: MEDLINE Main subject: Thiazoles / Hydrazones / Antineoplastic Agents / Nitrophenols Limits: Humans Language: En Year: 2018 Type: Article

Full text: 1 Database: MEDLINE Main subject: Thiazoles / Hydrazones / Antineoplastic Agents / Nitrophenols Limits: Humans Language: En Year: 2018 Type: Article