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.
Arylsulfonyl-N,N-diethyl-dithiocarbamates: a novel class of antitumor agents / A. Scozzafava;A. Mastrolorenzo;C. T. Supuran. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - STAMPA. - 10:(2000), pp. 1887-1891.
Arylsulfonyl-N,N-diethyl-dithiocarbamates: a novel class of antitumor agents.
SCOZZAFAVA, ANDREA;SUPURAN, CLAUDIU TRANDAFIR
2000
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.I documenti in FLORE sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.