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.
2005
273
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11581/202522
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