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

作者：Vasconcelos Zanair Soares; Lima Ralph Ana Carolina; Calcagno Danielle Queiroz; Barbosa Gleyce dos Santos; Pedrosa Tatiana do Nascimento; Antony Lucas Pio; Cardoso Smith Marllia de Arruda; Chazin Eliza de Lucas; Alves Vasconcelos Thatyana Rocha; Montenegro Raquel Carvalho; de Vasconcellos Marne Carvalho^*

来源：Toxicology in Vitro, 2018, 50: 225-235.

DOI：10.1016/j.tiv.2018.03.001

• AFN01
• B-RAF
• Cutaneous melanoma
• Cytotoxicity

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.

• 出版日期2018-8