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Benzo[b]thiophenesulphonamide 1,1-dioxide derivatives inhibit tNOX activity in a redox state-dependent manner

I Encío1, D J Morré, R Villar

  • 1Department of Health Sciences, Universidad Pública de Navarra, Avda. Barañain, 31008 Pamplona, Spain.

British Journal of Cancer
|February 3, 2005
PubMed

Insights

New benzo[b]thiophenesulphonamide 1,1-dioxide (BTS) derivatives show potent anticancer activity by inhibiting tumour-associated NADH oxidase (tNOX). This inhibition is redox-dependent, highlighting a novel therapeutic strategy for cancer treatment.

Area of Science:

  • Biochemistry
  • Pharmacology
  • Oncology

Background:

  • Benzo[b]thiophenesulphonamide 1,1-dioxide (BTS) derivatives are cytotoxic agents inducing reactive oxygen species (ROS) and apoptosis in tumor cells.
  • A correlation exists between BTS cytotoxicity and inhibition of plasma membrane tumour-associated NADH oxidase (tNOX) activity.
  • The precise origin of BTS-induced ROS remains unclear.

Purpose of the Study:

  • To synthesize and evaluate a novel BTS derivative for its cytotoxic and tNOX inhibitory activities.
  • To investigate the role of tNOX in BTS-induced ROS generation.
  • To analyze the influence of redox state on tNOX inhibition by the new BTS derivative.

Main Methods:

  • Synthesis of 6-[N-(2-phenylethyl)]benzo[b]thiophenesulphonamide 1,1-dioxide.
  • Assessment of cytotoxic activity against six human tumor cell lines (leukemia and solid tumors).
  • Evaluation of tNOX inhibitory activity under reducing and oxidizing conditions.

Main Results:

  • The novel BTS derivative exhibited strong cytotoxic activity across various human tumor cell lines.
  • The compound demonstrated potent inhibition of tNOX activity with an EC(50) of approximately 0.1 nM under reducing conditions (100 mM GSH).
  • tNOX inhibition was highly dependent on the redox state, showing no effect or slight stimulation under oxidizing conditions.

Conclusions:

  • The synthesized BTS derivative is a potent cytotoxic agent against human tumors.
  • The compound's efficacy is linked to the redox-dependent inhibition of tNOX.
  • This finding supports the targeting of tNOX as a potential anticancer strategy.

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