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2',3'-二脱氧-和2',3'-二脱氧-2',3'-二脱氢-腺苷及肌苷的噻吩并[3,4-d]嘧啶C-核苷类似物的合成与抗病毒评价

Synthesis and antiviral evaluation of thieno[3,4-d]pyrimidine C-nucleoside analogues of 2',3'-dideoxy- and 2',3'-dideoxy-2',3'-didehydro-adenosine and -inosine.

作者信息

Hamann Marie, Pierra Claire, Sommadossi Jean-Pierre, Musiu Chiara, Vargiu Luana, Liuzzi Michel, Storer Richard, Gosselin Gilles

机构信息

Idenix Pharmaceuticals, Medicinal Chemistry Laboratories IDENIX Sarl, Cap Gamma, 1682 rue de la Valsière, 34189 Montpellier Cedex 4, France.

出版信息

Bioorg Med Chem. 2009 Mar 15;17(6):2321-6. doi: 10.1016/j.bmc.2009.02.011. Epub 2009 Feb 14.

Abstract

Several thieno[3,4-d]pyrimidine derivatives, including four hitherto unknown 2',3'-dideoxy- and 2',3'-dideoxy-2',3'-didehydro-C-nucleoside analogues of adenosine and inosine have been synthesized. When evaluated in cell culture experiments against human immunodeficiency virus, none of the tested compounds exhibited any significant antiviral effect, while two of them showed some cytotoxicity.

摘要

已经合成了几种噻吩并[3,4-d]嘧啶衍生物,包括四种迄今未知的腺苷和肌苷的2',3'-二脱氧以及2',3'-二脱氧-2',3'-二脱氢-C-核苷类似物。在细胞培养实验中对这些化合物进行抗人免疫缺陷病毒评估时,所测试的化合物均未表现出任何显著的抗病毒作用,而其中两种显示出一定的细胞毒性。

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