2'-脱氧胞苷、2',3'-二脱氧尿苷和2',3'-二脱氧胞苷的一些5-硝基和5-氨基衍生物的合成及生物学评价

Synthesis and biological evaluation of some 5-nitro- and 5-amino derivatives of 2'-deoxycytidine, 2',3'-dideoxyuridine, and 2',3'-dideoxycytidine.

作者信息

Colacino Evelina, Sindona Giovanni, Gosselin Gilles, Mathé Christophe

机构信息

Laboratoire de Chimie Organique Biomoléculaire de Synthèse, UMR 5625 CNRS, Université Montpellier II, Montpellier, France.

出版信息

Nucleosides Nucleotides Nucleic Acids. 2003 Nov;22(11):2013-26. doi: 10.1081/NCN-120026403.

DOI:10.1081/NCN-120026403

PMID:14680024

Abstract

In this article, we describe the synthesis of 5-nitro-1-(2-deoxy-alpha-D-erythro-pentofuranosyl)cytosine (4alpha), 5-nitro-1-(2-deoxy-beta-D-erythro-pentofuranosyl)cytosine (4beta), 5-amino-1-(2-deoxy-alpha-D-erythro-pentofuranosyl)cytosine (5alpha), 5-nitro-1-(2-deoxy-beta-D-erythro-pentofuranosyl)cytosine (5beta), 5-nitro-1-(2,3-dideoxy-beta-D-ribofuranosyl)uracil (6beta), 5-amino-1-(2,3-dideoxy-alpha,beta-D-ribofuranosyl)uracil (7), 5-nitro-1-(2,3-dideoxy-alpha,beta-D-ribofuranosyl)cytosine (8) and 5-amino-1-(2,3-dideoxy-beta-D-ribofuranosyl)cytosine (9beta). The prepared compounds were tested for their activity against HIV and HBV viruses, but they did not show significant activity.

摘要

在本文中，我们描述了5-硝基-1-(2-脱氧-α-D-赤藓戊呋喃糖基)胞嘧啶(4α)、5-硝基-1-(2-脱氧-β-D-赤藓戊呋喃糖基)胞嘧啶(4β)、5-氨基-1-(2-脱氧-α-D-赤藓戊呋喃糖基)胞嘧啶(5α)、5-硝基-1-(2-脱氧-β-D-赤藓戊呋喃糖基)胞嘧啶(5β)、5-硝基-1-(2,3-二脱氧-β-D-核糖呋喃糖基)尿嘧啶(6β)、5-氨基-1-(2,3-二脱氧-α,β-D-核糖呋喃糖基)尿嘧啶(7)、5-硝基-1-(2,3-二脱氧-α,β-D-核糖呋喃糖基)胞嘧啶(8)和5-氨基-1-(2,3-二脱氧-β-D-核糖呋喃糖基)胞嘧啶(9β)的合成。对所制备的化合物进行了抗HIV和HBV病毒活性测试，但它们未显示出显著活性。