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Titolo:
Synthesis of unnatural 7-substituted-1-(2-deoxy-beta-D-ribofuranosyl)isocarbostyrils: "Thymine replacement" analogs of deoxythymidine for evaluation as antiviral and anticancer agents
Autore:
Naimi, E; Duan, WL; Wiebe, LI; Knaus, EE;
Indirizzi:
Univ Alberta, Fac Pharm & Pharmaceut Sci, Edmonton, AB T6G 2N8, Canada Univ Alberta Edmonton AB Canada T6G 2N8 Sci, Edmonton, AB T6G 2N8, Canada
Titolo Testata:
NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS
fascicolo: 8, volume: 20, anno: 2001,
pagine: 1533 - 1553
SICI:
1525-7770(2001)20:8<1533:SOU7>2.0.ZU;2-R
Fonte:
ISI
Lingua:
ENG
Soggetto:
THYMIDINE KINASE GENE; THYMIDYLATE SYNTHETASE; NUCLEOSIDE ANALOGS; DELIVERY SYSTEM; INHIBITION; THERAPY; MECHANISM; CELLS; BASE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
26
Recensione:
Indirizzi per estratti:
Indirizzo: Knaus, EE Univ Alberta, Fac Pharm & Pharmaceut Sci, Edmonton, AB T6G 2N8, Canada Univ Alberta Edmonton AB Canada T6G 2N8 ton, AB T6G 2N8, Canada
Citazione:
E. Naimi et al., "Synthesis of unnatural 7-substituted-1-(2-deoxy-beta-D-ribofuranosyl)isocarbostyrils: "Thymine replacement" analogs of deoxythymidine for evaluation as antiviral and anticancer agents", NUCLEOS NUC, 20(8), 2001, pp. 1533-1553

Abstract

A group of unnatural 1-(2-deoxy-beta -D-ribofuranosyl)isocarbostyrils having a variety of C-7 substituents [H, 4,7-(NO2)(2), I, CF3, CN, (E)-CH=CH-I,-C drop CH, -C dropC-I, -C dropC-Br, -C dropC-Me], designed as nucleoside mimics, were synthesized for evaluation as anticancer and antiviral agents. This class of compounds exhibited weak cytotoxicity in a MTT assay (CC50 =10(-3) to 10(-5) M range) with the 4,7-dinitro derivative being the most cytotoxic, relative to thymidine (CC50=10(-3) to 10(-5) M range), against a variety of cancer cell lines. The 4,7-dinitro, 7-I and 7-C drop CH compounds exhibited similar cytotoxicity against nontransfected (KBALB, 143B), and HSV-1 TK+ gene transfected (KBALB-STK, 143B-LTK) cancer cell lines possessing the herpes simplex virus type I (HSV-1) thymidine kinase gene (TK+). This observation indicates that these compounds are not substrates for HSV type-1 TK, and are therefore unlikely to be useful in gene therapy based on the HSV gene therapy paradigm.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 25/01/20 alle ore 15:46:13