On the design of polymeric 5′-O-ester prodrugs of 3′-azido-2′,3′-dideoxythymidine (AZT)

被引：20
|
作者：
Troev, Kolio D. [1 ]
Mitova, Violeta A. [1 ]
Ivanov, Ivan G. [2 ]
机构：
[1] Bulgarian Acad Sci, Inst Polymers, Sofia, Bulgaria
[2] Bulgarian Acad Sci, Inst Expt Pathol & Parasitol, Sofia, Bulgaria
来源：
TETRAHEDRON LETTERS | 2010年 / 51卷 / 47期
关键词：
Poly(oxyethylene H-phosphonate)s; Polymer conjugates; Anti-HIV prodrugs; Toxicity; AZT; 5'-O-HYDROGEN PHOSPHOLIPIDS; IMMOBILIZATION; AMINOTHIOLS;
D O I：
10.1016/j.tetlet.2010.09.076
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
A new 5'-O-AZT prodrug was synthesized by conjugating 3'-azido-2',3'-dideoxythymidine (AZT) with poly(oxyethylene H-phosphonate) at room temperature under Atherton-Todd reaction conditions. The acute toxicity of poly(5'-O-AZT-oxyethylene phosphate) was reduced significantly in comparison with non-immobilized AZT. (C) 2010 Elsevier Ltd. All rights reserved.
引用
收藏
页码：6123 / 6125
页数：3
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