Modulation of human mammary cell sensitivity to paclitaxel by new quinoline sulfonamides. |
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Authors: | K Chibale I Ojima H Haupt X Geng P Pera R J Bernacki |
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Institution: | Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa. chibale@science.uct.ac.za |
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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. |
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