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Identification of the novel N-phenylbenzenesulfonamide derivatives as potent HIV inhibitors

Yong Sun ,  Cui-Lin Lu ,  Chang-Yuan Wang ,  Rui-Rui Wang ,  Ke-Xin Liu ,  Liu-Meng Yang ,  Yu-Hong Zhen ,  Hou-Li Zhang ,  Chao Wang ,  Yong-Tang Zheng ,  Xiao-Dong Ma

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Citation:  Yong Sun, Cui-Lin Lu, Chang-Yuan Wang, Rui-Rui Wang, Ke-Xin Liu, Liu-Meng Yang, Yu-Hong Zhen, Hou-Li Zhang, Chao Wang, Yong-Tang Zheng, Xiao-Dong Ma. Identification of the novel N-phenylbenzenesulfonamide derivatives as potent HIV inhibitors[J]. Chinese Chemical Letters, 2015, 26(2): 243-247. doi: 10.1016/j.cclet.2014.11.004 shu

Identification of the novel N-phenylbenzenesulfonamide derivatives as potent HIV inhibitors

    • 通讯作者: Yong-Tang Zheng,
    Xiao-Dong Ma,
  • 基金项目:

    This work was supported in part by grants from the National Natural Science Foundation of China (No. 81402788) (No. 81402788)

    the Ph.D. Start-up Fund of Natural Science Foundation of Liaoning Province, China (No. 20141115). (No. 20141115)

摘要: Searching for more safe and effective agents for HIV treatments is still an urgent topic worldwide. Based on our continuous modifications on the benzophenone derivatives as HIV-1 reverse transcriptase (RT) inhibitors, a new template bearing N-phenylbenzenesulfonamide (PBSA) structure was designed to enhance the interactions with HIV-1 RT. In this manuscript, a series of PBSA derivatives were synthesized and evaluated for their anti-HIV-1 activity. The preliminary test showed that these compounds were potent to inhibit wild-type HIV-1 with EC50 values ranging of 0.105-14.531 mmol/L. In particular, compound 13f not only has high anti-HIV-1 activity (0.108 mmol/L), but also possesses low toxicity with a TI value of 1816.6. Furthermore, the major interactions of the inhibitor 13f with HIV-1 RT were also investigated using the molecular modelling. Our discovered structure-activity relationships (SARs) of these analogues may serve as an important clue for further optimizations.

English

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  • 发布日期:  2014-11-10
  • 收稿日期:  2014-09-02
  • 网络出版日期:  2014-10-23
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