Seley-Radtke Katherine L, Sunkara Naresh K
Department of Chemistry and Biochemistry, University of Maryland Baltimore County, Baltimore, Maryland, USA.
Nucleosides Nucleotides Nucleic Acids. 2009 May;28(5):633-41. doi: 10.1080/15257770903091920.
The discovery of azidothymidine's (AZT) activity against human immunodeficiency virus (HIV) provided strong rationale for the design of additional thymidine analogues. One drawback of many nucleoside analogues is the toxicity that often arises due to phosphorylation by cellular kinases. In order to overcome this problem, a number of truncated nucleosides lacking the 4'-hydroxymethyl group have been synthesized. In that regard, the synthesis and preliminary biological results for two truncated carbocyclic thymidine analogues are presented herein.
叠氮胸苷(AZT)对人类免疫缺陷病毒(HIV)活性的发现为设计更多胸苷类似物提供了有力依据。许多核苷类似物的一个缺点是由于细胞激酶磷酸化常常产生毒性。为了克服这个问题,已经合成了许多缺少4'-羟甲基的截短核苷。在这方面,本文介绍了两种截短的碳环胸苷类似物的合成及初步生物学结果。