Design, Synthesis and Biological Evaluation of Substituted Guanidine Indole Derivatives as Potential Inhibitors of HIV-1 Tat-TAR Interaction

Author(s): Jun Wang, Yan Wang, Zhenyu Li, Peng Zhan, Rujun Bai, Christophe Pannecouque, Jan Balzarini, Erik De Clercq, Xinyong Liu

Journal Name: Medicinal Chemistry

Volume 10 , Issue 7 , 2014

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The interaction between the HIV-1 transactivator protein Tat and RNA response element (TAR) plays a critical role in HIV-1 transcription. Based on the pharmacophore model of reported inhibitors, a series of novel substituted guanidine indole derivatives was designed, synthesized and evaluated for their in vitro HIV-1 and HIV-2 inhibitory activity using the IIIB strain and ROD strain, respectively. Preliminary biological evaluation indicated that three compounds exhibited marked inhibitory activity against HIV-1 IIIB. Quite unexpectedly, compound a-7 was also endowed with the moderate anti-HIV-2 potency (EC50 = 58.14 µM). In addition, preliminary discussion on the activity results and molecular modeling of these new analogues were presented in this manuscript.

Keywords: Drug design, guanidine indole synthesis, HIV-1 Tat, HIV-1 TAR, inhibitors.

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Article Details

Year: 2014
Published on: 22 September, 2014
Page: [738 - 746]
Pages: 9
DOI: 10.2174/1573406410666140306151815
Price: $65

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