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Anti-AIDS agents 87. New bio-isosteric dicamphanoyl-dihydropyranochromone (DCP) and dicamphanoyl-khellactone (DCK) analogues with potent anti-HIV activity  期刊论文  

  • 编号:
    4982ce2b-022f-4d63-934c-3a97be5c6551
  • 作者:
    Liu, HongShan[1];Xu, ShiQing[1];Cheng, Ming[1];Chen, Ying(陈瑛)*[1]Xia, Peng(夏鹏)[1]Qian, Keduo[2];Xia, Yi[2];Yang, ZhengYu[2];Chen, ChinHo[3];MorrisNatschke, Susan L.[2];Lee, KuoHsiung[2,4];
  • 语种:
    English
  • 期刊:
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS ISSN:0960-894X 2011 年 21 卷 19 期 (5831 - 5834) ; OCT 1
  • 收录:
  • 关键词:
  • 摘要:

    Six 3'R,4'R-di-O-(S)-camphanoyl-2',2'-dimethyldihydropyrano[2,3-f] chromone (DCP) and two 3'R,4'R-di-O-(S)-camphanoyl-(+)-cis-khellactone (DCK) derivatives were designed, synthesized, and evaluated for inhibition of HIV-1(NL4-3) replication in TZM-bl cells. 2-Ethyl-2'-monomethyl-1'-oxa- and -1'-thia-DCP (5a, 6a), as well as 2-ethyl-1'-thia-DCP (7a) exhibited potent anti-HIV activity with EC(50) values of 30, 38 and 54 nM and therapeutic indexes of 152.6, 48.0 and 100.0, respectively, which were better than or comparable to those of the lead compound 2-ethyl-DCP in the same assay. 4-Methyl-1'-thia-DCK (8a) also showed significant inhibitory activity with an EC(50) of 128 nM and TI of 237.9. (C) 2011 Elsevier Ltd. All rights reserved.

  • 推荐引用方式
    GB/T 7714:
    Liu Hong-Shan,Xu Shi-Qing,Cheng Ming, et al. Anti-AIDS agents 87. New bio-isosteric dicamphanoyl-dihydropyranochromone (DCP) and dicamphanoyl-khellactone (DCK) analogues with potent anti-HIV activity [J].BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2011,21(19):5831-5834.
  • APA:
    Liu Hong-Shan,Xu Shi-Qing,Cheng Ming,Chen Ying,&Lee Kuo-Hsiung.(2011).Anti-AIDS agents 87. New bio-isosteric dicamphanoyl-dihydropyranochromone (DCP) and dicamphanoyl-khellactone (DCK) analogues with potent anti-HIV activity .BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,21(19):5831-5834.
  • MLA:
    Liu Hong-Shan, et al. "Anti-AIDS agents 87. New bio-isosteric dicamphanoyl-dihydropyranochromone (DCP) and dicamphanoyl-khellactone (DCK) analogues with potent anti-HIV activity" .BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 21,19(2011):5831-5834.
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