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.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Antimalarials / chemistry
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Antimalarials / pharmacology
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Antineoplastic Agents / chemistry*
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Antineoplastic Agents / pharmacology*
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Antineoplastic Agents, Phytogenic / pharmacology
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Breast Neoplasms / drug therapy*
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Drug Design
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Drug Resistance, Multiple
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Drug Resistance, Neoplasm
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Drug Screening Assays, Antitumor
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Humans
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Inhibitory Concentration 50
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Models, Molecular
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Paclitaxel / pharmacology*
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Quinolines / chemistry
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Structure-Activity Relationship
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Sulfonamides / chemistry
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Sulfonamides / pharmacology
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Tumor Cells, Cultured
Substances
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Antimalarials
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Antineoplastic Agents
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Antineoplastic Agents, Phytogenic
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Quinolines
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Sulfonamides
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quinoline
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Paclitaxel