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新型非核苷类HIV逆转录酶抑制剂DCK的研究进展 被引量:2

Progress in the new nonnucleoside anti-HIV reverse transcriptase inhibitor-DCK
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摘要 DCK是以天然产物为先导化合物经结构修饰得到的一个高活性抗HIV化合物,其作用机制独特,不同于现有的非核苷类逆转录酶抑制剂,高效低毒,有可能发展成为一类新的抗HIV药物。近年来以它为先导化合物进行了多方面的结构修饰,以期得到药用性质更好的化合物。本文就DCK的发现、结构修饰、构效关系及最新进展予以介绍。 3' ,4'-Di-O-(S)-comphanoyl-( + )-c/s-khellactone (DCK) is a synthetic khellactone ester that exhibits potent anti-HIV activity with a mechanism distinct from clinically used anti-HIV agents. Several series of DCK analoges have been synthesized and evaluated for inhibitory effects against HIV. This review article describes recent progress in the discovery, structural modification, and structure-activity relationship studies of potent anti-HIV DCK derivatives.
作者 郭焕芳 谢蓝
出处 《药学学报》 CAS CSCD 北大核心 2008年第10期997-1002,共6页 Acta Pharmaceutica Sinica
基金 北京市科委"针对重大疾病的创新药物研究"专项基金资助项目(D0204003041631)
关键词 DCK 非核苷类逆转录酶抑制剂 艾滋病 人类免疫缺陷病毒 DCK nonnucleoside anti-HIV reverse transcriptase inhibitor AIDS HIV
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参考文献22

  • 1Gallo RC, Sarin PS, Gelmann EP, et al. Isolation of human T-celll eukemiavirus in acquired immune deficiency syndrome (AIDS) [ J ]. Science, 1983,220: 865 - 867.
  • 2FDA. Antiretroviral drugs approved by FDA for HIV. Information may be found at internet at: http://www. fda. gov/oashi/aids/virals, html/.
  • 3Lee TT, Kashiwada Y, Huang L, et al. Suksdorfin: An anti-HIV principle from Lomatium suksdorfii, its structure-activity correlation with related coumarins, and synergistic effects with anti-AIDS nucleosides [ J ]. Bioorg Med Chem Lett, 1994,2:1051 -1056.
  • 4Huang L, KashiwadaY, Cosentino LM, et al. 3',4'-Di- O-( - )-camphanoyl-( + )-cis-khellactone and related compounds: a new class of potent anti-HIV agents [ J]. Bioorg Med Chem Lett, 1994,4:593 - 598.
  • 5Huang L, KashiwadaY, Cosentino LM, et al. Anti-AIDS agents. 15. Synthesis and anti-HIV activity of dihydroseselins and related analogs [ Jl. J Med Chem, 1994,37:3947 - 3955.
  • 6Huang L, Yuan X, Yu DL, et al. Mechanism of action and resistant profile of anti-HIV-1 coumarin derivatives [ J ]. Virology, 2005,332:623 - 628.
  • 7Xie L, Crimmins MT, Lee KH. Anti-AIDS agents. 22. Asymmetric synthesis of 3', 4'-di-O-( - )-camphanoyl- ( + )-cis-khellactone (DCK), a potent anti-HIV agent [ J ]. Tetrahedron Lett, 1995,36:4529 - 4532.
  • 8Kolb HC, Van Nieuwenhze MS, Sharpless KB. Catalytic asymmetric dihydroxylation [ J]. Chem Rev (Washington DC, US), 1994,94:2483 - 2547.
  • 9Xie L, Takeuchi Y, Cosentino LM, et al. Anti-AIDS agents. 37. Synthesis and structure-activity relationships of (3'R,4'R)-( + )-cis-khellactone derivatives as novel potent anti-HIV agents [ J]. J Med Chem, 1999,42: 2662 - 2672.
  • 10Xie L, Takeuchi Y, CosentinoLM, et al. Anti-AIDS agents 33 synthesis and anti-HIV activity of mono-methyl substituted 3', 4'-di-O-( - )-camphanoyl-( + )-cis- khellactone (DCK) analogs [ J]. Bioorg Med Chem Lett, 1998,8:2151 -2156.

同被引文献19

  • 1Marx J. L: Science[J], 1982, 217(4560) : 618-621.
  • 2Gallo R. C. , Salahuddin S. Z. , Popovic M. , Shearer G. M. , Kaplan M. , Haynes B. F. , Palker T. J. , Oleske Redfield R. J. , Safai B: Science[J] , 1984, 224(4648) : 500-503.
  • 3Barre-Sinoussi F. , Chermann J. C. , Rey F. , Nugeyre M. T. , Chamaret S. , Gruest J. , Dauguet C. , Axler-Blin C. , Vezinet-Brun F. , Rouzioux C. , Rozenbaum W. , Montagnier L: Science[J], 1983, 220(4599) : 868-871.
  • 4Ravichandran V. , Mourya V. K. , Agrawal R. K: Intemet Electronic Journal of Molecular Design[ J], 2007, 6 (11 ) : 363-374.
  • 5YoungS. D., BritcherS. F., TranL. O., PayneL. S., LummaW. C., LyleT. A., HuffJ. R., AndersonP. S., Olsen D. B., Carroll S. S: Anti Microbial Agents and Chemotherapy[ J], 1995, 39(12) : 2602-2605.
  • 6Sustiva(Efavirenz) Drug Capsule and Tablet Product Information[ Z, Bristol-Myers Squibb Company, NJ08543, USA, 2011.
  • 7Hyperchem Release 6.0[ CP] , Gainesville, Hypercube Inc. , 2000.
  • 8Dewar M. J. S., Zoebisch E. G., Healy E. F., Stewart J. J. P: J. Am. Chem. Soc. [J], 1985, 107(13):3902-3909.
  • 9Frisch M. J. , Trucks G. W. , Schlegel H. B. , Scuseria G. E. , Robb M. A. , Cheeseman J. R. , Zakrzewski V. G. , Montgomery J. A. Jr. , Stratmann R. E. , Burant J. C. , Dapprich S. , Millam J. M. , Daniels A. D. , Kudin K. N. , Strain M. C. , Farkas O. , Tomasi J. , Barone V. , Cossi M. , Cammi R. , Mennucci B. , Pomelli C. , Adamo C. , Clifford S. , Ochterski J. , Petersson G. A. , Ayala P. Y. , Cui Q. , Morokuma K. , Malick D. K. , Rabuck A. D. , Raghavachari K. , Foresman J. B. , Cioslowski J. , Ortiz J. V. , Stefanov B. B. , Liu G. , Liashenko A. , Piskorz P. , Komaromi I. , Gomperts R. , Martin R. L. , Fox D. J. , Keith T. , A1-Laham M. A. , Peng C. Y. , Nanayakkara A. , Gonzalez C. , Challacomhe M. , Gill P. M. W. , Johnson B. G. ,Chen W. , Wong M. W. , Andres J. L. , Head-Gordon M. , Replogle E. S., Pople J. A: Gaussian 98, Revision A. 9 [ CP], Pittsburgh PA: Gaussian Inc. , 1998.
  • 10YEDe-Yong(叶德泳).计算机辅助药物设计导论[M],Bering:ChemicalIndustry Press,2003:43-49.

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