Adenosine derivatives modified at the 1-, 2-, or 3-C-position of the ribose ring by the introduction of a methyl group were evaluated for their antitumor activity. 3'-C-Methyladenosine (3'-Me-Ado) showed the higher cytotoxicity compared to that of other analogues against human myelogenous leukemia K562, human colon carcinoma HT-29, and human breast carcinoma MCF-7 cell lines. Structure-activity relationships study showed that the structure of 3'-Me-Ado is crucial for the activity. The cytotoxicity of 3'-Me-Ado could be explained by its ability to reduce the levels of both intracellular purine and pyrimidine deoxynucleotides through ribonucleotide reductase (RR) inhibition.
The antitumor effects of 3’-methyl-adenosine mediated by inhibition of ribonucleotide reductase.
CAPPELLACCI, Loredana;PETRELLI, Riccardo;
2005-01-01
Abstract
Adenosine derivatives modified at the 1-, 2-, or 3-C-position of the ribose ring by the introduction of a methyl group were evaluated for their antitumor activity. 3'-C-Methyladenosine (3'-Me-Ado) showed the higher cytotoxicity compared to that of other analogues against human myelogenous leukemia K562, human colon carcinoma HT-29, and human breast carcinoma MCF-7 cell lines. Structure-activity relationships study showed that the structure of 3'-Me-Ado is crucial for the activity. The cytotoxicity of 3'-Me-Ado could be explained by its ability to reduce the levels of both intracellular purine and pyrimidine deoxynucleotides through ribonucleotide reductase (RR) inhibition.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
