Synthesis, characterisation and potent cytotoxicity of unconventional platinum(iv) complexes with modified lipophilicity?

Dalton Transactions Pub Date: 2019-10-16 DOI: 10.1039/C9DT03339D

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.

Graphical abstract: Synthesis, characterisation and potent cytotoxicity of unconventional platinum(iv) complexes with modified lipophilicity
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