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  • Title: Synthesis, characterisation and potent cytotoxicity of unconventional platinum(iv) complexes with modified lipophilicity.
    Author: Deo KM, Sakoff J, Gilbert J, Zhang Y, Aldrich Wright JR.
    Journal: Dalton Trans; 2019 Nov 26; 48(46):17217-17227. PubMed ID: 31729519.
    Abstract:
    Novel platinum(iv) complexes were synthesised to examine the facile modulation of the lipophilicity of the complex by incorporating axial ligands of increasing length, ranging from 2-6 carbons. RP-HPLC was used to establish the lipophilicity of each complex. The in vitro cytotoxicities of all complexes were determined against a panel of malignant cell lines and a non-cancerous cell line. While there was no clear correlation between lipophilicity and cytotoxicity, all complexes demonstrated nanomolar activity against all cell lines. The most potent complexes exhibited 850-fold greater activity than cisplatin against HT29 colon carcinoma with GI50 values of 13 nM.
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