CD4 mimics targeting the HIV entry mechanism and their hybrid molecules with a CXCR4 antagonist
CD4 mimics targeting the HIV entry mechanism and their hybrid molecules with a CXCR4 antagonist
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DOI：
10.1016/j.bmcl.2010.07.106
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发表时间：
2010-10-01
影响因子：
2.7
通讯作者：
Tamamura, Hirokazu
中科院分区：
文献类型：
--
作者：
Narumi, Tetsuo;Ochiai, Chihiro;Tamamura, Hirokazu
CD4模拟物的小分子先前被报道为HIV-1进入抑制剂，阻断gp120-CD4相互作用并诱导gp120的构象变化，暴露其共受体结合位点。我们对一系列CD4模拟类似物进行了结构-活性关系（SAR）研究，以探讨CD4模拟物1的哌啶部分对抗hiv活性、细胞毒性和CD4模拟物对gp120构象变化的影响。此外，还合成了几种基于CD4模拟物与选择性CXCR4拮抗剂偶联的杂交分子，并对其效用进行了评估。(C) 2010 Elsevier Ltd.版权所有。
Small molecules behaving as CD4 mimics were previously reported as HIV-1 entry inhibitors that block the gp120-CD4 interaction and induce a conformational change in gp120, exposing its co-receptor-binding site. A structure-activity relationship (SAR) study of a series of CD4 mimic analogs was conducted to investigate the contribution from the piperidine moiety of CD4 mimic 1 to anti-HIV activity, cytotoxicity, and CD4 mimicry effects on conformational changes of gp120. In addition, several hybrid molecules based on conjugation of a CD4 mimic analog with a selective CXCR4 antagonist were also synthesized and their utility evaluated. (C) 2010 Elsevier Ltd. All rights reserved.