Cytotoxic Titanium(IV) Complexes of Salalen-Based Ligands

Avia Tzubery, Edit Y. Tshuva*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

25 Scopus citations

Abstract

A new family of cytotoxic TiIV complexes is described, based on the salalen (half salan and half salen) ligands. Altogether, 17 (salalen)TiIV complexes with different ligand substitutions and different numbers of labile groups were synthesized. Representative complexes were characterized by X-ray crystallography. The complexes were evaluated for their hydrolytic stability in 10 % D2O solutions, their cytotoxicity toward HT-29 human colon cancer cells, and the retaining of activity after pre-incubation in aquatic medium prior to cell addition. The results showed that: (a) reducing complexes' lability increased hydrolytic stability, (b) bulky groups often increased kinetic stability toward hydrolysis, but also damaged accessibility, (c) for unstable complexes, some hydrolysis products are likely the active species, (d) specific hydrophobic groups may facilitate penetration through the cell membrane, and (e) one di-tert-butylated salalen catecholato complex was identified as the superior derivative, combing high cytotoxicity with high stability and accessibility.

Original languageAmerican English
Pages (from-to)1695-1705
Number of pages11
JournalEuropean Journal of Inorganic Chemistry
Volume2017
Issue number12
DOIs
StatePublished - 27 Mar 2017

Bibliographical note

Publisher Copyright:
© 2017 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim

Keywords

  • Antitumor agents
  • Cisplatin
  • Cytotoxicity
  • O ligands
  • Salalen
  • Solid-state structures
  • Structure–activity relationships
  • Titanium

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