Chin. J. Org. Chem. ›› 2018, Vol. 38 ›› Issue (5): 1267-1270.DOI: 10.6023/cjoc201710033 Previous Articles     Next Articles



郭叶a, 傅莉莉b, 范晓文a, 史宣玲b   

  1. a 包头医学院药学院 包头 014060;
    b 清华大学医学院 艾滋病综合研究中心 北京 100084
  • 收稿日期:2017-10-25 修回日期:2018-01-08 发布日期:2018-01-18
  • 通讯作者: 史宣玲,
  • 基金资助:


Synthesis and Anti-HIV-1 Activity of Stapled HIV-1 Fusion Inhibitors

Guo Yea, Fu Lilib, Fan Xiaowena, Shi Xuanlingb   

  1. a School of Pharmacy, Baotou Medical College, Baotou 014060;
    b Comprehensive AIDS Research Center, School of Medicine, Tsinghua University, Beijing 100084
  • Received:2017-10-25 Revised:2018-01-08 Published:2018-01-18
  • Contact: 10.6023/cjoc201710033
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 21602121), the Natural Science Foundation of Inner Mongolia (No. 2016BS0201) and the Doctoral Science Foundation of Baotou Medical College (No. BSJJ201620).

Sifuvirtide (SFT) is a potent anti-HIV-1 (human immunodeficiency virus-1) fusion inhibitor and it shows higher potency and pharmacokinetic stability than the approved fusion inhibitor T20. At present, sifuvirtide has completed the phase Ⅱb clinical trial in China. In this study, SFT-1 and SFT-2 were synthesized via all-hydrocarbon cross-linking system with replacing the original salt bridge in SFT by hydrocarbon covalent bond, using sifuvirtide as template. The anti-HIV-1 activity was evaluated for all synthetic peptides. The results indicated that SFT stapled peptides displayed high inhibitory activity against seven HIV-1 pseudovirus strains, and SFT-1 showed the highest inhibitory activity against B' and B'C subtype virus strains, SFT-2 showed the highest inhibitory activity against B, CRF01_AE and CRF08_BC subtype virus strains.

Key words: sifuvirtide, HIV-1 fusion inhibitor, hydrocarbon stapling, anti-HIV-1 activity