title: Modulation of human mammary cell sensitivity to paclitaxel by new quinoline sulfonamides.
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.
authors.affiliation: Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa. chibale@science.uct.ac.za
authors.forename: K
authors.initials: K
authors.lastname: Chibale
authors.forename: I
authors.initials: I
authors.lastname: Ojima
authors.forename: H
authors.initials: H
authors.lastname: Haupt
authors.forename: X
authors.initials: X
authors.lastname: Geng
authors.forename: P
authors.initials: P
authors.lastname: Pera
authors.forename: R J
authors.initials: RJ
authors.lastname: Bernacki
mesh_terms: D000962:Antimalarials / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D000972:Antineoplastic Agents, Phytogenic / Q000494:pharmacology; D001943:Breast Neoplasms / Q000188:drug therapy*; D015195:Drug Design; D018432:Drug Resistance, Multiple; D019008:Drug Resistance, Neoplasm; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020128:Inhibitory Concentration 50; D008958:Models, Molecular; D017239:Paclitaxel / Q000494:pharmacology*; D011804:Quinolines / Q000737:chemistry; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000737:chemistry / Q000494:pharmacology; D014407:Tumor Cells, Cultured
chemical_list: D000962:Antimalarials; D000970:Antineoplastic Agents; D000972:Antineoplastic Agents, Phytogenic; D011804:Quinolines; D013449:Sulfonamides; C037219:quinoline; D017239:Paclitaxel