The design, synthesis, and biological evaluation of novel substituted purines as HIV-1 Tat-TAR inhibitors |
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Authors: | Yuan Dekai He Meizi Pang Ruifang Lin Shrong-Shi Li Zhengming Yang Ming |
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Institution: | National Research Laboratory of Natural and Biomimetic Drugs, Peking University Health Science Center, Beijing 100083, PR China. |
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Abstract: | 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. |
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