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Updated: Feb 12, 2026

DNAzyme-dependent Analysis of rRNA 2’-O-Methylation
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Anticancer potential of benzothiazolic derivative (E)-2-((2-(benzo[d]thiazol-2-yl)hydrazono)methyl)-4-nitrophenol

Zanair Soares Vasconcelos1, Ana Carolina Lima Ralph1, Danielle Queiroz Calcagno2

  • 1Faculty of Pharmaceutical Sciences, Federal University of Amazon, Amazon, Brazil.

Toxicology in Vitro : an International Journal Published in Association with BIBRA
|March 26, 2018
PubMed

Insights

A novel benzothiazole derivative, AFN01, shows significant antitumor activity against human melanoma cells. This compound induces DNA damage and apoptosis, inhibiting melanoma cell proliferation, migration, and invasion, suggesting its therapeutic potential.

Area of Science:

  • Oncology
  • Molecular Biology
  • Medicinal Chemistry

Background:

  • Malignant melanoma is an aggressive cancer with a poor prognosis, driving research into targeted therapies.
  • Frequently mutated genes (NRAS, B-RAF, TP53) are key targets for advanced melanoma treatments.
  • Benzothiazole derivatives have demonstrated antitumor potential.

Purpose of the Study:

  • To evaluate the antitumor activity of the benzothiazole derivative (E)-2-((2-(benzo[d]thiazol-2-yl)hydrazono)methyl)-4-nitrophenol (AFN01).
  • To assess AFN01's effects on human melanoma cell lines with TP53, NRAS, and B-RAF mutations.
  • To investigate AFN01's mechanism of action, including DNA damage and apoptosis induction.

Main Methods:

  • Utilized three human melanoma cell lines representing common genetic alterations (TP53, NRAS, B-RAF).
  • Assessed the cytostatic and cytotoxic effects of AFN01.
  • Investigated AFN01's impact on DNA integrity, cell proliferation, migration, invasion, and apoptosis.

Main Results:

  • AFN01 demonstrated significant cytostatic and cytotoxic effects on melanoma cell lines.
  • AFN01 induced DNA fragmentation, including single and double-strand breaks.
  • AFN01 inhibited cell proliferation, migration, and invasion, correlating with apoptosis induction.

Conclusions:

  • AFN01 exhibits potent antitumor activity against human melanoma cells.
  • The mechanism involves DNA damage and apoptosis, leading to reduced cell proliferation and metastasis.
  • AFN01 represents a promising therapeutic candidate for melanoma treatment.
Keywords:
AFN01B-RAFCutaneous melanomaCytotoxicity

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