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Biotinylated Pt(IV) prodrugs with elevated lipophilicity and cytotoxicity.

Daniil SpectorAlexander S ErofeevPeter GorelkinDmitry A SkvortsovAlexander TrigubAlina MarkovaVita NikitinaNikolay V Ul'yanovskiiAlexander Shtil'Alevtina SemkinaKsenia VlasovaNikolay ZykAlexander MajougaElena K BeloglazkinaOlga O Krasnovskaya
Published in: Dalton transactions (Cambridge, England : 2003) (2023)
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.
Keyphrases
  • cancer therapy
  • induced apoptosis
  • single cell
  • ionic liquid
  • cell proliferation
  • oxidative stress
  • long non coding rna
  • endoplasmic reticulum stress