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2000
Volume 10, Issue 7
  • ISSN: 1573-4064
  • E-ISSN: 1875-6638

Abstract

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 'M). In addition, preliminary discussion on the activity results and molecular modeling of these new analogues were presented in this manuscript.

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/content/journals/mc/10.2174/1573406410666140306151815
2014-11-01
2025-05-29
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/content/journals/mc/10.2174/1573406410666140306151815
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  • Article Type:
    Research Article
Keyword(s): Drug design; guanidine indole synthesis; HIV-1 TAR; HIV-1 Tat; inhibitors
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