Anticancer potential of benzothiazolic derivative (E)-2-((2-(benzo[d]thiazol-2-yl)hydrazono)methyl)-4-nitrophenol against melanoma cells.

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.

• Authors: Zanair Soares Vasconcelos, Ana Carolina Lima Ralph, Danielle Queiroz Calcagno, Gleyce Dos Santos Barbosa, Tatiana do Nascimento Pedrosa, Lucas Pio Antony, Marília de Arruda Cardoso Smith, Eliza de Lucas Chazin, Thatyana Rocha Alves Vasconcelos, Raquel Carvalho Montenegro, Marne Carvalho de Vasconcellos
• Journal: Toxicology in vitro : an international journal published in association with BIBRA (Toxicol In Vitro) Vol. 50 Pg. 225-235 (Aug 2018) ISSN: 1879-3177 [Electronic] England
• PMID: 29574239 (Publication Type: Journal Article)
• Copyright: Copyright © 2018 Elsevier Ltd. All rights reserved.

Chemical References

• (E)-2-((2-(benzo(d)thiazol-2-yl)hydrazono)methyl)-4-nitrophenol
• Antineoplastic Agents
• Hydrazones
• Membrane Proteins
• Nitrophenols
• TP53 protein, human
• Thiazoles
• Tumor Suppressor Protein p53
• BRAF protein, human
• Proto-Oncogene Proteins B-raf
• GTP Phosphohydrolases
• NRAS protein, human

Topics

• Antineoplastic Agents (pharmacology)
• Cell Line, Tumor
• Cell Movement (drug effects)
• Cell Survival (drug effects)
• DNA Fragmentation
• GTP Phosphohydrolases (genetics)
• Humans
• Hydrazones (pharmacology)
• Melanoma (drug therapy, genetics)
• Membrane Proteins (genetics)
• Nitrophenols (pharmacology)
• Proto-Oncogene Proteins B-raf (genetics)
• Thiazoles (pharmacology)
• Tumor Suppressor Protein p53 (genetics)
• Wound Healing (drug effects)