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Anti-AIDS agents 82: Synthesis of seco-(3 ' R,4 ' R)-3 ',4 '-di-O-(S)-camphanoyl-(+)-cis-khellactone (DCK) derivatives as novel anti-HIV agents 期刊论文

编号：

6af45341-3f77-4d9e-9aaf-31a4e412cf95
作者：

Tang, Jian^[1];Qian, Keduo^[2];Zhang, BeiNa(张蓓娜)^[1]Chen, Ying(陈瑛)*^[1]Xia, Peng(夏鹏)^[1]Yu, Donglei^[2];Xia, Yi^[2];Yang, ZhengYu^[2];Chen, ChinHo^[3];MorrisNatschke, Susan L.^[2];Lee, KuoHsiung^[2];
语种：

English
期刊：

BIOORGANIC & MEDICINAL CHEMISTRY ISSN：0968-0896 2010 年 18 卷 12 期 (4363 - 4373) ; JUN 15
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关键词：

Seco-DCK analogs Anti-HIV agents
摘要：

Thirteen novel seco-DCK analogs (4-16) with several new skeletons were designed, synthesized and screened for in vitro anti-HIV-1 activity. Among them, three compounds (5, 13, and 16) showed moderate activity, and compound 9 exhibited the best activity with an EC(50) value of 0.058 mu M and a therapeutic index (TI) of 1000. The activity of 9 was better than that of 4-methyl DCK (2, EC(50): 0.126 mu M, TI: 301.2) in the same assay. Additionally, 9 also showed antiviral activity against a multi-RT inhibitor-resistant strain (RTMDR), which is insensitive to most DCK analogs. Compared with 2, compound 9 has a less complex structure, fewer hydrogen-bond acceptors, and a reduced log P value. Therefore, it is likely to exhibit better ADME, and appears to be a promising new lead for further development as an anti-HIV candidate. (C) 2010 Elsevier Ltd. All rights reserved.
推荐引用方式
GB/T 7714：

Tang Jian,Qian Keduo,Zhang Bei-Na, et al. Anti-AIDS agents 82: Synthesis of seco-(3 ' R,4 ' R)-3 ',4 '-di-O-(S)-camphanoyl-(+)-cis-khellactone (DCK) derivatives as novel anti-HIV agents [J].BIOORGANIC & MEDICINAL CHEMISTRY,2010,18(12):4363-4373.
APA：

Tang Jian,Qian Keduo,Zhang Bei-Na,Chen Ying,&Lee Kuo-Hsiung.(2010).Anti-AIDS agents 82: Synthesis of seco-(3 ' R,4 ' R)-3 ',4 '-di-O-(S)-camphanoyl-(+)-cis-khellactone (DCK) derivatives as novel anti-HIV agents .BIOORGANIC & MEDICINAL CHEMISTRY,18(12):4363-4373.
MLA：

Tang Jian, et al. "Anti-AIDS agents 82: Synthesis of seco-(3 ' R,4 ' R)-3 ',4 '-di-O-(S)-camphanoyl-(+)-cis-khellactone (DCK) derivatives as novel anti-HIV agents" .BIOORGANIC & MEDICINAL CHEMISTRY 18,12(2010):4363-4373.

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