2'-叠氮-2'-脱氧尿苷和2'-叠氮-2'-脱氧胞苷的生物活性及磷酸化作用

Biological activity and phosphorylation of 2'-azido-2'-deoxyuridine and 2'-azido-2'-deoxycytidine.

作者信息

Kang S H, Cho M J

机构信息

School of Pharmacy, University of North Carolina, Chapel Hill 27514, USA.

出版信息

Nucleosides Nucleotides. 1998 Jun;17(6):1077-88. doi: 10.1080/07328319808004221.

DOI:10.1080/07328319808004221

PMID:9708323

Abstract

2'-Azido-2'-deoxyuridine and 2'-azido-2'-deoxycytidine were evaluated for their inhibitory activity against ribonucleotide reductase and for subsequent cell growth inhibition. Their mono- and di-phosphates were synthesized and their inhibitory activities against the reductase were also determined in a permeabilized cell system, along with the two nucleosides. The results of the present study identify the first phosphorylation step involved in the conversion of the two azidonucleosides to the corresponding diphosphates to be rate-limiting in the overall activation.

摘要

对2'-叠氮基-2'-脱氧尿苷和2'-叠氮基-2'-脱氧胞苷进行了评估，以研究它们对核糖核苷酸还原酶的抑制活性以及随后对细胞生长的抑制作用。合成了它们的单磷酸盐和二磷酸盐，并在透化细胞系统中测定了它们对还原酶的抑制活性，同时也测定了这两种核苷的抑制活性。本研究结果表明，将两种叠氮核苷转化为相应二磷酸盐的第一步磷酸化反应是整个激活过程中的限速步骤。