The design, synthesis, and biological evaluation of novel substituted purines as HIV-1 Tat–TAR inhibitors
| Autor: | Shrong-Shi Lin, Zheng-Ming Li, Ruifang Pang, Dekai Yuan, Meizi He, Ming Yang |
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| Rok vydání: | 2007 |
| Předmět: |
Models
Molecular Transcriptional Activation Magnetic Resonance Spectroscopy Molecular model Anti-HIV Agents Stereochemistry viruses Clinical Biochemistry Pharmaceutical Science Microbial Sensitivity Tests Giant Cells Sensitivity and Specificity Biochemistry Cell Line Structure-Activity Relationship Transactivation Tar (tobacco residue) Drug Discovery Side chain Animals Humans Purine metabolism Molecular Biology Cell Proliferation HIV Long Terminal Repeat Syncytium Molecular Structure Chemistry Organic Chemistry HEK 293 cells RNA Stereoisomerism Protein Structure Tertiary Purines Drug Design Gene Products tat Molecular Medicine |
| Zdroj: | Bioorganic & Medicinal Chemistry. 15:265-272 |
| ISSN: | 0968-0896 |
| DOI: | 10.1016/j.bmc.2006.09.062 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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