Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 23, Issue 24, Pages 7521-7528Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2015.10.039
Keywords
Dual-action HIV-1 Integrase/Reverse; Transcriptase inhibitors; Baylis-Hillman reaction; 3-Hydroxy-3-phenylpropanoate esters; Cinnamate esters; Azidothymidine (AZT)
Funding
- South African Medical Research Council (MRC)
- National Treasury under its Economic Competitiveness and Support Package
- MRC
- Rhodes University
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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. (C) 2015 Elsevier Ltd. All rights reserved.
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