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Titolo:
Arylsulfonyl-N,N-dialkyl-dithiocarbamates as tumor cell growth inhibitors:Novel agents targeting beta-tubulin?
Autore:
Scozzafava, A; Mastrolorenzo, A; Supuran, CT;
Indirizzi:
Univ Florence, Lab Chim Inorgan & Bioinorgan, I-50121 Florence, Italy UnivFlorence Florence Italy I-50121 Bioinorgan, I-50121 Florence, Italy Univ Florence, Dipartimento Sci Dermatol, Ctr MTS, I-50122 Florence, ItalyUniv Florence Florence Italy I-50122 l, Ctr MTS, I-50122 Florence, Italy
Titolo Testata:
JOURNAL OF ENZYME INHIBITION
fascicolo: 1, volume: 16, anno: 2001,
pagine: 55 - 63
SICI:
8755-5093(2001)16:1<55:AATCGI>2.0.ZU;2-O
Fonte:
ISI
Lingua:
ENG
Soggetto:
CARBONIC-ANHYDRASE INHIBITORS; ANTITUMOR AGENT; CANCER-CELLS; IN-VIVO; SULFONAMIDES; EFFICACY; BINDING;
Keywords:
N,N-dialkyl-dithiocarbamates; arylsulfonyl-N,N-dialkyl-dithiocarbamates; tubulin; antitumor agent;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
22
Recensione:
Indirizzi per estratti:
Indirizzo: Supuran, CT Univ Florence, Lab Chim Inorgan & Bioinorgan, Via Gino Capponi7, I-50121 Florence, Italy Univ Florence Via Gino Capponi 7 Florence Italy I-50121 Italy
Citazione:
A. Scozzafava et al., "Arylsulfonyl-N,N-dialkyl-dithiocarbamates as tumor cell growth inhibitors:Novel agents targeting beta-tubulin?", J ENZ INHIB, 16(1), 2001, pp. 55-63

Abstract

Reaction of sodium N,N-dimethyldithiocarbamate or N,N-diethyldithiocarbamate with arylsulfonyl halides afforded a series of arylsulfonyl-N,N-dialkyldithiocarbamates. The reactivity of these new derivatives with cysteine and glutathione has been investigated in order to identify derivatives that might label a cysteine residue of the heterodimeric protein tubulin which plays a critical physiological function in cell division and also possesses enzymatic activity as a GTP-ase. Since many antitumor drugs exert their actionby binding to tubulin, inhibiting in this way microtubule association and provoking cell death, some of the most reactive compounds against the thiolreagents found in this work have been assayed for their antitumor activity. Indeed strong tumor cell growth inhibitory properties against several leukemia, non-small cell lung, ovarian, melanoma, colon, CNS, renal, prostate and breast cancer has been found in vitro for some of the 4-halogeno-, 4-methyl- or 4-carboxyphenyl-substituted arylsulfonyl-N,N-dialkyl-dithiocarbamates. Furthermore, some of these derivative were shown to act as in vitro tubulin polymerization inhibitors using a turbidimetric assay.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 22/01/20 alle ore 12:59:14