Synthesis and anti-cancer activity of some novel 5-azacytosine nucleosides

Tiwari, K. N.; Cappellacci, Loredana; Montgomery, J. A.; Iii, Secrist J. A.

doi:10.1081/NCN-120026872

1-O-Acetyl-2-deoxy-3,5-di-O-toluoyl-4-thio-D-erythro-pentofuranose and 2-deoxy-1,3,5-tri-O-acetyl-4-thio-L-threo-pentofuranose were coupled with 5-azacytosine to obtain α and β anomers of nucleosides. All four nucleosides were reduced to the corresponding dihydro derivatives and deblocked to give target compounds. All eight target compounds were evaluated in a series of human cancer cell lines in culture. Only 2′-deoxy-4′ -thio-5-azacytidine (3β) was found to be cytotoxic in all the cell lines and was further evaluated in vivo. Details of the synthesis and biological activity are reported.

Scheda prodotto non validato

Attenzione! I dati visualizzati non sono stati sottoposti a validazione da parte dell'ateneo

Titolo:	Synthesis and anti-cancer activity of some novel 5-azacytosine nucleosides
Autori:	TIWARI K. N. CAPPELLACCI, Loredana MONTGOMERY J. A. SECRIST J. A. III mostra contributor esterni nascondi contributor esterni
Data di pubblicazione:	2003
Rivista:	NUCLEOSIDES, NUCLEOTIDES & NUCLEIC ACIDS
Abstract:	1-O-Acetyl-2-deoxy-3,5-di-O-toluoyl-4-thio-D-erythro-pentofuranose and 2-deoxy-1,3,5-tri-O-acetyl-4-thio-L-threo-pentofuranose were coupled with 5-azacytosine to obtain α and β anomers of nucleosides. All four nucleosides were reduced to the corresponding dihydro derivatives and deblocked to give target compounds. All eight target compounds were evaluated in a series of human cancer cell lines in culture. Only 2′-deoxy-4′ -thio-5-azacytidine (3β) was found to be cytotoxic in all the cell lines and was further evaluated in vivo. Details of the synthesis and biological activity are reported.
Handle:	http://hdl.handle.net/11581/112702
Appare nelle tipologie:	Articolo

File in questo prodotto:

Non ci sono file associati a questo prodotto.

Utilizza questo identificativo per citare o creare un link a questo documento:
http://hdl.handle.net/11581/112702

Citazioni

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.