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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / metabolism
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Antineoplastic Agents / pharmacology*
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Colchicine / pharmacology
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Cysteine / chemistry
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Dose-Response Relationship, Drug
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Drug Screening Assays, Antitumor
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Female
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Glutathione / chemistry
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Humans
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Kinetics
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Male
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Molecular Structure
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Sulfonamides / chemical synthesis*
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Sulfonamides / chemistry
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Sulfonamides / metabolism
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Sulfonamides / pharmacology*
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Thiocarbamates / chemical synthesis*
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Thiocarbamates / chemistry
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Thiocarbamates / metabolism
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Thiocarbamates / pharmacology*
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Tubulin / chemistry
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Tubulin / metabolism
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Tumor Cells, Cultured
Substances
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Antineoplastic Agents
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Sulfonamides
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Thiocarbamates
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Tubulin
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Glutathione
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Cysteine
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Colchicine