Anti-AIDS agents 88. Anti-HIV conjugates of betulin and betulinic acid with AZT prepared via click chemistry

被引：71

作者：

Bori, Ibrahim D. ^{[1
]}

Hung, Hsin-Yi ^{[1
]}

Qian, Keduo ^{[1
]}

Chen, Chin-Ho ^{[2
]}

Morris-Natschke, Susan L. ^{[1
]}

Lee, Kuo-Hsiung ^{[1
,3
]}

机构：

[1] Univ N Carolina, UNC Eshelman Sch Pharm, Nat Prod Res Labs, Chapel Hill, NC 27599 USA

[2] Duke Univ, Med Ctr, Dept Surg, Durham, NC 27710 USA

[3] China Med Univ & Hosp, Chinese Med Res & Dev Ctr, Taichung 401, Taiwan

来源：

TETRAHEDRON LETTERS | 2012年 / 53卷 / 15期

关键词：

Betulin; Betulinic acid; AZT; Anti-HIV; Click chemistry; INHIBITOR; BEVIRIMAT; SAFETY; PHARMACOKINETICS; DERIVATIVES; MATURATION; PA-457;

D O I：

10.1016/j.tetlet.2012.02.022

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

In the present study, a new strategy to link AZT with betulin/betulinic acid (BA) by click chemistry was designed and achieved. This conjugation via a triazole linkage offers a new direction for the modification of anti-HIV triterpenes. Click chemistry provides an easy and productive way for linking two molecules, even when one of them is a large natural product. Among the newly synthesized conjugates, compounds 15 and 16 showed potent anti-HIV activity with EC50 values of 0.067 and 0.10 mu M, respectively, which are comparable to that of AZT (EC50: 0.10 mu M) in the same assay. (C) 2012 Elsevier Ltd. All rights reserved.

引用

页码：1987 / 1989

页数：3

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