title: Arylsulfonyl-N,N-diethyl-dithiocarbamates: a novel class of antitumor agents.
abstract: A series of alkyl/arylsulfonyl-N,N-diethyl-dithiocarbamates has been prepared by reaction of sodium N,N-diethyldithiocarbamate with alkyl/arylsulfonyl halides. The reactivity of these new derivatives against cysteine and glutathione has been investigated in order to identify derivatives that might label a critical cysteine residue of tubulin (Cys 239 of human beta2 tubulin chain). Some of the most reactive compounds showed moderate to powerful tumor growth inhibitory properties against several leukemia, non-small cell lung, ovarian, melanoma, colon, CNS, renal, prostate and breast cancer cell lines in vitro.
authors.affiliation: Università degli Studi, Laboratorio di Chimica Inorganica e Bioinorganica, Florence, Italy.
authors.forename: A
authors.initials: A
authors.lastname: Scozzafava
authors.forename: A
authors.initials: A
authors.lastname: Mastrolorenzo
authors.forename: C T
authors.initials: CT
authors.lastname: Supuran
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D003078:Colchicine / Q000494:pharmacology; D003545:Cysteine / Q000737:chemistry; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D005260:Female; D005978:Glutathione / Q000737:chemistry; D006801:Humans; D007700:Kinetics; D008297:Male; D015394:Molecular Structure; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D013859:Thiocarbamates / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D014404:Tubulin / Q000737:chemistry / Q000378:metabolism; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D013449:Sulfonamides; D013859:Thiocarbamates; D014404:Tubulin; D005978:Glutathione; D003545:Cysteine; D003078:Colchicine