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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. 2015
Meloddy H Manyeruke, and
Temitope O Olomola, and
Swarup Majumder, and
Shaakira Abrahams, and
Michelle Isaacs, and
Nicodemus Mautsa, and
Salerwe Mosebi, and
Dumisani Mnkandhla, and
Raymond Hewer, and
Heinrich C Hoppe, and
Rosalyn Klein, and
Perry T Kaye
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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