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    Antitumor platinum(IV) derivatives of carboplatin and the histone deacetylase inhibitor 4-phenylbutyric acid

    Almotairy, Awatif Rashed Z. and Gandin, Valentina and Morrison, Liam and Marzano, Cristina and Montagner, Diego and Erxleben, Andrea (2017) Antitumor platinum(IV) derivatives of carboplatin and the histone deacetylase inhibitor 4-phenylbutyric acid. Journal of Inorganic Biochemistry, 177. pp. 1-7. ISSN 0162-0134

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    Five new platinum(IV) derivatives of carboplatin each incorporating the histone deacetylase inhibitor 4-phenylbutyrate in axial position were synthesized and characterized by 1H and 195Pt NMR spectroscopy, electrospray ionization mass spectrometry and elemental analysis, namely cis,trans-[Pt(CBDCA)(NH3)2(PBA)(OH)] (1), cis,trans-[Pt(CBDCA)(NH3)2(PBA)2] (2), cis,trans-[Pt(CBDCA)(NH3)2(PBA)(bz)] (3), cis,trans-[Pt(CBDCA)(NH3)2(PBA)(suc)] (4) and cis,trans-[Pt(CBDCA)(NH3)2)(PBA)(ac)] (5) (PBA = 4-phenylbutyrate, CBDCA = 1,1-cyclobutane dicarboxylate, bz = benzoate, suc = succinate and ac = acetate). The reduction behavior in the presence of ascorbic acid was studied by high performance liquid chromatography. The cytotoxicity against a panel of human tumor cell lines, histone deacetylase (HDAC) inhibitory activity, cellular accumulation and the ability to induce apoptosis were evaluated. The most effective complex, compound 3, was found to be up to ten times more effective than carboplatin and to decrease cellular basal HDAC activity by approximately 18% in A431 human cervical cancer cells.

    Item Type: Article
    Keywords: Anticancer; Carboplatin; Histone deacetylase inhibitor; 4-Phenylbutyric acid; Platinum(IV);
    Academic Unit: Faculty of Science and Engineering > Chemistry
    Faculty of Science and Engineering > Research Institutes > Human Health Institute
    Item ID: 11672
    Identification Number:
    Depositing User: Diego Montagner
    Date Deposited: 12 Nov 2019 12:41
    Journal or Publication Title: Journal of Inorganic Biochemistry
    Publisher: Elsevier
    Refereed: Yes
    Use Licence: This item is available under a Creative Commons Attribution Non Commercial Share Alike Licence (CC BY-NC-SA). Details of this licence are available here

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