Bioorganic & Medicinal Chemistry Letters 28 (2018) 1067–1070 Contents lists available at ScienceDirect Bioorganic & Medicinal Chemistry Letters journal homepage: www.elsevier.com/locate/bmcl Synthesis and evaluation of substituted 4-arylimino-3-hydroxybutanoic acids as potential HIV-1 integrase inhibitors a c c b,c a,c,⇑ Faridoon , Dumisani Mnkandhla , Michelle Isaacs , Heinrich C. Hoppe , Perry T. Kaye Department of Chemistry, Rhodes University, Grahamstown 6140, South Africa Department of Biochemistry and Microbiolgy, Rhodes University, Grahamstown 6140, South Africa Centre for Chemico- and Biomedicinal Research, Rhodes University, Grahamstown 6140, South Africa article i nfo abstract Article history: A series of readily accessible 4-arylimino-3-hydroxybutanoic acids have been prepared and evaluated as Received 6 November 2017 potential HIV-1 Integrase inhibitors. None of the ligands exhibited signiﬁcant toxicity against human Revised 29 January 2018 embryonic kidney (HEK 293) cells, while ﬁve of them showed activity against HIV-1 integrase – the most Accepted 10 February 2018 active (6c) with an IC value of 3.5 lM. In silico docking studies indicate the capacity of ligand 6c to inter- Available online 12 February 2018 2+ act with several amino acid residues and the two Mg cations in the HIV-1 integrase receptor cavity. 2018 Published by Elsevier Ltd. Keywords: HIV-1 integrase inhibitors
Bioorganic & Medicinal Chemistry Letters – Elsevier
Published: Apr 1, 2018
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