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Synthesis and evaluation of 3-hydroxy-3-phenylpropanoate ester–AZT conjugates as potential dual-action HIV-1 Integrase and Reverse Transcriptase inhibitors.
- Source :
-
Bioorganic & medicinal chemistry [Bioorg Med Chem] 2015 Dec 15; Vol. 23 (24), pp. 7521-8. - Publication Year :
- 2015
-
Abstract
- Novel 3-hydroxy-3-phenylpropanoate ester-azidothymidine (AZT) conjugates have been prepared using Baylis-Hillman methodology, and their potential as dual-action HIV-1 Integrase and Reverse Transcriptase inhibitors has been explored using enzyme inhibition and computer modelling techniques; their activity and HeLa cell toxicity have been compared with those of their cinnamate ester analogues.
- Subjects :
- Anti-HIV Agents
HIV Infections drug therapy
HIV Infections virology
HIV Integrase metabolism
HIV Integrase Inhibitors chemical synthesis
HIV Reverse Transcriptase antagonists & inhibitors
HIV Reverse Transcriptase metabolism
HIV-1 enzymology
HeLa Cells
Humans
Molecular Docking Simulation
Reverse Transcriptase Inhibitors chemical synthesis
Structure-Activity Relationship
Zidovudine chemical synthesis
HIV Integrase Inhibitors chemistry
HIV Integrase Inhibitors pharmacology
HIV-1 drug effects
Reverse Transcriptase Inhibitors chemistry
Reverse Transcriptase Inhibitors pharmacology
Zidovudine chemistry
Zidovudine pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3391
- Volume :
- 23
- Issue :
- 24
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 26775541
- Full Text :
- https://doi.org/10.1016/j.bmc.2015.10.039