کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1362055 | 981477 | 2007 | 8 صفحه PDF | دانلود رایگان |

A series of novel substituted purines containing a side chain with a terminal amino or guanidyl group were designed and synthesized as HIV-1 Tat–TAR inhibitors. All the compounds could effectively block the TAR transactivation in human 293T cells with the CAT expression percentage ranging from 34.4% to 65.7% and showed high antiviral effects with low cytotoxicities in inhibiting the formation of SIV-induced syncytium in CEM174 cells. Molecular modeling studies by Auto-dock process suggest that the compounds bind to TAR RNA in two different modes.
Substituted purines containing a side chain with a terminal amino or guanidyl group were designed and synthesized as HIV-1 Tat–TAR inhibitors. Title compounds possessed high inhibitory activity and modeling suggests that they bind to TAR in two different modes.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry - Volume 15, Issue 1, 1 January 2007, Pages 265–272