New cytotoxic benzo(b)thiophenilsulfonamide 1,1-dioxide derivatives inhibit a NADH oxidase located in plasma membranes of tumour cells.
A series of benzo(b)thiophenesulfonamide 1,1-dioxide derivatives (BTS) have been designed and synthesized as candidate antineoplastic drugs. Several of these compounds have shown in vitro cytotoxic activity on leukaemic CCRF-CEM cells. The cytotoxic BTS, but not the inactive ones, were able to inhibit a tumour cell-specific NADH oxidase activity present in the membrane of CCRF-CEM cells.
Alonso
M M
MM
Department of Health Sciences, Public University of Navarra, Avd Barañaín s/n, Pamplona, 31008, Spain.
Encío
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I
Martínez-Merino
V
V
Gil
M
M
Migliaccio
M
M
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D002462:Cell Membrane / Q000187:drug effects / Q000201:enzymology; D003470:Culture Media; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007700:Kinetics; D007938:Leukemia / Q000473:pathology; D009097:Multienzyme Complexes / Q000037:antagonists & inhibitors* / Q000378:metabolism; D009247:NADH, NADPH Oxidoreductases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013453:Sulfonylurea Compounds / Q000138:chemical synthesis / Q000494:pharmacology*; D013876:Thiophenes / Q000138:chemical synthesis / Q000494:pharmacology*; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D003470:Culture Media; D009097:Multienzyme Complexes; D013453:Sulfonylurea Compounds; D013876:Thiophenes; C088015:benzothiophene; C023107:NADH oxidase; D009247:NADH, NADPH Oxidoreductases