Synthesis of 5-alkynylated d4T analogues as potential HIV-1 reverse transcriptase inhibitors

被引：4

作者：

Ciurea, A

Fossey, C

Gavriliu, D

Delbederi, Z

Sugeac, E

Laduree, D

Schmidt, S

Laumond, G

Aubertin, AM

机构：

[1] Univ Caen, UFR Sci Pharmaceut, Ctr Etud & Rech Med Normandie, F-14032 Caen, France

[2] INSERM, F-67000 Strasbourg, France

来源：

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | 2004年 / 19卷 / 06期

关键词：

HIV; reverse transcriptase; d4T analogues; alkynyl tether; Sonogashira;

D O I：

10.1080/14756360412331280527

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of 2',3'-didehydro-2',3'-dideoxynucleosides substituted with an alkynylhydroxy- (6, 7, 12 and 13) and alkynylamino- (20) groups at the C-5 position were synthesized. All these five target modified nucleosides were tested for anti-human immunodeficiency virus type 1 activity in CEM-SS and MT-4 cells and unfortunately displayed no improvement in antiviral activity.

引用

收藏

页码：511 / 519

页数：9

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