Modulation of human mammary cell sensitivity to paclitaxel by new quinoline sulfonamides

  • Bioorg Med Chem Lett. 2001 Sep 17;11(18):2457-60. doi: 10.1016/s0960-894x(01)00462-0.
K Chibale  1 ,  I Ojima ,  H Haupt ,  X Geng ,  P Pera ,  R J Bernacki
Affiliations
  • 1. Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa. [email protected]
PMID: 11549446 DOI: 10.1016/s0960-894x(01)00462-0
Abstract

Sulfonamide derivatives of chloroquine and primaquine were synthesised and evaluated against both paclitaxel-sensitive and paclitaxel-resistant mammarian Cancer cell lines. All derivatives exhibited at least 96% MDR reversal activity when co-administered with paclitaxel at 5 microM. The best compound, a chloroquine derivative, exhibited 99% MDR reversal activity when co-administered with paclitaxel at 1 microM. Molecular modelling studies reveal that these derivatives share a common pharmacophore with taxane MDR reversal agents.