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. 2023 Jan 24;52(4):866-871.
doi: 10.1039/d2dt03662b.

Biotinylated Pt(IV) prodrugs with elevated lipophilicity and cytotoxicity

Daniil Spector  1   2 , Alexander Erofeev  1   2 , Peter Gorelkin  1   2 , Dmitry Skvortsov  1 , Alexander Trigub  3 , Alina Markova  4 , Vita Nikitina  1 , Nikolay Ul'yanovskiy  5 , Alexander Shtil'  6 , Alevtina Semkina  7   8 , Ksenia Vlasova  1   8 , Nikolay Zyk  1 , Alexander Majouga  9 , Elena Beloglazkina  1 , Olga Krasnovskaya  1   2
Affiliations

Biotinylated Pt(IV) prodrugs with elevated lipophilicity and cytotoxicity

Daniil Spector et al. Dalton Trans. .

Abstract

A design of Pt(IV) prodrugs with tumor cell targeting moieties leading to increased selectivity is of interest. Herein, we designed a novel Pt(IV) prodrugs with COX-inhibitor naproxen, long-chain hydrophobic stearic acid moiety and biotin as axial ligands. We have established that for Pt(IV) prodrugs with biotin and naproxen or stearate in axial position, the lipophilicity rather than biotin receptors expression is the main factor of cytotoxicity. We also monitored the reduction speed of Pt(IV) prodrug 3 with naproxen and biotin in axial positions in A549 cells using XANES and demonstrated that the prodrug gradually releases cisplatin within 20 hours of incubation.

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