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ID: ALA1133953

Journal: Bioorg Med Chem Lett

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

Authors: Chibale K, Ojima I, Haupt H, Geng X, Pera P, Bernacki RJ.

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.

CiteXplore: 11549446

DOI: 10.1016/s0960-894x(01)00462-0