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Anti-AIDS agents. Part 62: Anti-HIV activity of 2 '-substituted 4-methyl-3 ',4 '-di-O-(-)-camphanoyl-(+)-cis-khellactone (4-methyl DCK) analogs  期刊论文  

  • 编号:
    ae53dfb5-d0a2-4184-ad17-37b9ea648c6a
  • 作者:
    Zhang, Q(张倩); Chen, Y;Xia, P;Xia, Y;Yang, ZY;Yu, DL;MorrisNatschke, SL;Lee, KH;
  • 语种:
    English
  • 期刊:
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS ISSN:0960-894X 2004 年 14 卷 23 期 (5855 - 5857) ; DEC 6
  • 收录:
  • 摘要:

    Four 4-methyl-3',4'-di-O-(-)-camphanoyl-(+)-cis-khellactone (4-methyl DCK) analogs (7a-d) with different alkyl substituents at the 2'-position were synthesized and evaluated for inhibition of HIV-1 replication in H9 lymphocytes. 2'-Methyl-2'ethyl-4-methyl DCK (7b) was more potent (EC50 = 0.22muM TI > 175) than the other three compounds (7a, 7c, and 7d), but significantly less potent than 4-methyl DCK (2, EC50 = 0.0059muM, TI > 6600). The bioassay results indicated that the 2'-substituents had a strong effect on the anti-HIV activity, and gem-dimethyl substitution at the 2'-position was greatly preferable to larger alkyl substituents or hydrogen atoms. (C) 2004 Elsevier Ltd. All rights reserved.

  • 推荐引用方式
    GB/T 7714:
    Zhang Q,Chen Y,Xia P, et al. Anti-AIDS agents. Part 62: Anti-HIV activity of 2 '-substituted 4-methyl-3 ',4 '-di-O-(-)-camphanoyl-(+)-cis-khellactone (4-methyl DCK) analogs [J].BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2004,14(23):5855-5857.
  • APA:
    Zhang Q,Chen Y,Xia P,Xia Y,&Lee KH.(2004).Anti-AIDS agents. Part 62: Anti-HIV activity of 2 '-substituted 4-methyl-3 ',4 '-di-O-(-)-camphanoyl-(+)-cis-khellactone (4-methyl DCK) analogs .BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,14(23):5855-5857.
  • MLA:
    Zhang Q, et al. "Anti-AIDS agents. Part 62: Anti-HIV activity of 2 '-substituted 4-methyl-3 ',4 '-di-O-(-)-camphanoyl-(+)-cis-khellactone (4-methyl DCK) analogs" .BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 14,23(2004):5855-5857.
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