Synthesis and evaluation of 3-hydroxy-3-phenylpropanoate ester­AZT conjugates as potential dual-action HIV-1 Integrase and Reverse Transcriptase inhibitors.

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.