Synthesis and biological activity of novel N6-substituted and 2,N6-disubstituted adenine ribo- and 3'-C-methyl-ribonucleosides as antitumor agents

Cappellacci, Loredana; Petrelli, Riccardo; Franchetti, Palmarisa; Vita, Patrizia; Kusumanchi, P; Kumar, M; Jayaram, H. N.; Zhou, B; Yen, Y; Grifantini, Mario

A series of N6-aminopurine-9-b-D-ribonucleosides and ribose-modified 30-C-methyl analogues substituted at N6-position with a small group like hydroxy, methoxy or amino group or at C2(N6) position have been synthesized and tested against a panel of human leukemia and carcinoma cell lines. N6- Hydrazino-9-b-D-ribofuranosyl-purine (5) displayed the best antiproliferative activity in the low micromolar or submicromolar range against all tested tumor cell lines. The activity of this nucleoside is related in part to ribonucleotide reductase inhibition. C2-modification or 30-C-methylation in N6- substituted adenosine analogues leads to a decrease or loss in activity.

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Titolo:	Synthesis and biological activity of novel N6-substituted and 2,N6-disubstituted adenine ribo- and 3'-C-methyl-ribonucleosides as antitumor agents
Autori:	CAPPELLACCI, Loredana PETRELLI, Riccardo FRANCHETTI, Palmarisa VITA, PATRIZIA Kusumanchi P Kumar M Jayaram H. N. Zhou B Yen Y GRIFANTINI, Mario mostra contributor esterni nascondi contributor esterni
Data di pubblicazione:	2011
Rivista:	EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Abstract:	A series of N6-aminopurine-9-b-D-ribonucleosides and ribose-modified 30-C-methyl analogues substituted at N6-position with a small group like hydroxy, methoxy or amino group or at C2(N6) position have been synthesized and tested against a panel of human leukemia and carcinoma cell lines. N6- Hydrazino-9-b-D-ribofuranosyl-purine (5) displayed the best antiproliferative activity in the low micromolar or submicromolar range against all tested tumor cell lines. The activity of this nucleoside is related in part to ribonucleotide reductase inhibition. C2-modification or 30-C-methylation in N6- substituted adenosine analogues leads to a decrease or loss in activity.
Handle:	http://hdl.handle.net/11581/218562
Appare nelle tipologie:	Articolo

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