Novel halogenated sulfonamides inhibit the growth of multidrug resistant MCF-7/ADR cancer cells

  • Bioorg Med Chem Lett. 1999 Jul 5;9(13):1843-6. doi: 10.1016/s0960-894x(99)00276-0.
J C Medina  1 ,  D Roche ,  B Shan ,  R M Learned ,  W P Frankmoelle ,  D L Clark ,  T Rosen ,  J C Jaen
Affiliations
  • 1. Tularik Inc., South San Francisco, CA 94080, USA.
PMID: 10406652 DOI: 10.1016/s0960-894x(99)00276-0
Abstract

In this report, we describe the synthesis of halogenated benzenesulfonamide compounds and their ability to inhibit the growth of HeLa, MCF-7 and MCF-7/ADR tumor cells in vitro. The multidrug resistance (MDR) phenotype of certain cells does not affect their sensitivity to these compounds. These agents belong to a family of compounds previously shown to bind irreversibly to cysteine-239 of beta-tubulin. Consistent with this mechanism of action, the cytotoxicities of these compounds appear to correlate with their ability to undergo nucleophilic aromatic substitution.