Gold(I) complex of 1,1′-bis(diphenylphosphino) ferrocene–quinoline conjugate : a virostatic agent against HIV-1

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dc.contributor.author Gama, Ntombenhle
dc.contributor.author Kumar, Kamlesh
dc.contributor.author Ekengard, Erik
dc.contributor.author Haukka, Matti
dc.contributor.author Darkwa, James
dc.contributor.author Nordlander, Ebbe
dc.contributor.author Meyer, Debra
dc.date.accessioned 2016-06-24T06:23:21Z
dc.date.issued 2016-06
dc.description.abstract HIV infection is known for replication in proliferating CD+ T-cells. Treatment of these cells with cytostatic (anti-proliferation) compounds such as hydroxyurea interferes with the cells’s ability support HIV replication. Combinations of such cytostatic compounds with proven anti-retroviral drugs (like ddI) are known as virostatic , and have been shown to aid in the control of the infection. The use of two different drugs in virostatic combinations however, carries the risk of adverse effects including drug-drug interactions, which could lead to augmented toxicities and reduced efficacy. Here, a novel digold(I) complex of ferrocenequinoline (3) was investigated for cytostatic behaviour as well as anti-viral activity which if demonstrated would eliminate concerns of drug-drug interactions. The complex was synthesized and characterized by NMR, FT-IR and mass spectroscopy and the molecular structure was confirmed by X-ray crystallography. Bio-screening involved viability dyes, real time electronic sensing and whole virus assays. The complex showed significant (p = 0.0092) inhibition of virus infectivity (83%) at 10 ug/mL. This same concentration caused cytostatic behaviour in TZM-bl cells with significant (p<0.01) S and G2/M phase cell cycle arrest. These data supports 3 as a virostatic agent, possessing both anti-viral and cytostatic characteristics. en_ZA
dc.description.department Biochemistry en_ZA
dc.description.embargo 2017-06-30
dc.description.librarian hb2016 en_ZA
dc.description.sponsorship National Research Foundation (NRF) and the Technology Innovation Agency (TIA), South Africa. NRF Innovation Doctoral Scholarship. European Commission (Erasmus Mundus Europe Asia, EMEA) and University of Johannesburg, South Africa en_ZA
dc.description.uri http://link.springer.com/journal/10534 en_ZA
dc.identifier.citation Gama, N, Kumar, K, Ekengard, E, Haukka, M, Darkwa, J, Nordlander, E & Meyer, D 2016, 'Gold(I) complex of 1,1′-bis(diphenylphosphino) ferrocene–quinoline conjugate : a virostatic agent against HIV-1', BioMetals, vol. 29, no. 3, pp. 389-397 en_ZA
dc.identifier.issn 0966-0844 (print)
dc.identifier.issn 1572-8773 (online)
dc.identifier.other 10.1007/s10534-016-9921-9
dc.identifier.uri http://hdl.handle.net/2263/53384
dc.language.iso en en_ZA
dc.publisher Springer en_ZA
dc.rights © Springer Science+Business Media New York 2016. The original publication is available at : http://link.springer.com/journal/10534. en_ZA
dc.subject HIV infection en_ZA
dc.subject Hydroxyurea interferes en_ZA
dc.subject Cytostatic (anti-proliferation) compounds en_ZA
dc.subject Human immunodeficiency virus (HIV) en_ZA
dc.title Gold(I) complex of 1,1′-bis(diphenylphosphino) ferrocene–quinoline conjugate : a virostatic agent against HIV-1 en_ZA
dc.type Postprint Article en_ZA


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