title: Synthesis and evaluation of 3-hydroxy-3-phenylpropanoate ester–AZT 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.
authors.forename: Meloddy H
authors.initials: MH
authors.lastname: Manyeruke
authors.forename: Temitope O
authors.initials: TO
authors.lastname: Olomola
authors.forename: Swarup
authors.initials: S
authors.lastname: Majumder
authors.forename: Shaakira
authors.initials: S
authors.lastname: Abrahams
authors.forename: Michelle
authors.initials: M
authors.lastname: Isaacs
authors.forename: Nicodemus
authors.initials: N
authors.lastname: Mautsa
authors.forename: Salerwe
authors.initials: S
authors.lastname: Mosebi
authors.forename: Dumisani
authors.initials: D
authors.lastname: Mnkandhla
authors.forename: Raymond
authors.initials: R
authors.lastname: Hewer
authors.forename: Heinrich C
authors.initials: HC
authors.lastname: Hoppe
authors.forename: Rosalyn
authors.initials: R
authors.lastname: Klein
authors.forename: Perry T
authors.initials: PT
authors.lastname: Kaye
mesh_terms: D019380:Anti-HIV Agents; D015658:HIV Infections / Q000188:drug therapy / Q000821:virology; D019427:HIV Integrase / Q000378:metabolism; D019428:HIV Integrase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors / Q000378:metabolism; D015497:HIV-1 / Q000187:drug effects* / Q000201:enzymology; D006367:HeLa Cells; D006801:Humans; D062105:Molecular Docking Simulation; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D015215:Zidovudine / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D019380:Anti-HIV Agents; D019428:HIV Integrase Inhibitors; D018894:Reverse Transcriptase Inhibitors; D015215:Zidovudine; D019427:HIV Integrase; D054303:HIV Reverse Transcriptase; C514801:p31 integrase protein, Human immunodeficiency virus 1