Publication date: Available online 31 October 2015
Source:Bioorganic & Medicinal Chemistry
Author(s): Meloddy H. Manyeruke, Temitope O. Olomola, Swarup Majumder, Shaakira Abrahams, Michelle Isaacs, Nicodemus Mautsa, Salerwe Mosebi, Dumisani Mnkandhla, Raymond Hewer, Heinrich C. Hoppe, Rosalyn Klein, 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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