Synthesis and evaluation of 3-hydroxy-3-phenylpropanoate ester–AZT conjugates as potential dual-action HIV-1 Integrase and Reverse Transcriptase inhibitors

Add time:09/02/2019    Source:sciencedirect.com

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.

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