Trans titanium(IV) complexes of salen ligands exhibit high antitumor activity

Avia Tzubery; Edit Y. Tshuva

doi:10.1021/ic201296h

Trans titanium(IV) complexes of salen ligands exhibit high antitumor activity

Avia Tzubery, Edit Y. Tshuva^*

^*Corresponding author for this work

Institute of Chemistry

Research output: Contribution to journal › Article › peer-review

43 Scopus citations

Abstract

Salen-titanium(IV) complexes are introduced as a new family of highly efficient antitumor complexes, being the first cytotoxic titanium(IV) complexes of trans labile ligands, as characterized crystallographically. Four complexes with different aromatic substitutions were analyzed, reveling a meaningful effect of the ligand structure on the complex performance. All complexes exhibit high hydrolytic stability, where the labile OAr ligands hydrolyze in a 10% D ₂O solution with t _1/2 ranging from 2 to 11 h. The IC ₅₀ values obtained for three of the salen complexes studied on HT-29 colon and OVCAR-1 ovarian cells demonstrate activity that exceeds those of the known tianium(IV) complexes Cp ₂TiCl ₂ and (bzac) ₂Ti(OiPr) ₂ and that of cisplatin, where the most active para-chlorinated complex exhibits activity enhancement relative to cisplatin by 10-fold.

Original language	English
Pages (from-to)	7946-7948
Number of pages	3
Journal	Inorganic Chemistry
Volume	50
Issue number	17
DOIs	https://doi.org/10.1021/ic201296h
State	Published - 5 Sep 2011

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abstract = "Salen-titanium(IV) complexes are introduced as a new family of highly efficient antitumor complexes, being the first cytotoxic titanium(IV) complexes of trans labile ligands, as characterized crystallographically. Four complexes with different aromatic substitutions were analyzed, reveling a meaningful effect of the ligand structure on the complex performance. All complexes exhibit high hydrolytic stability, where the labile OAr ligands hydrolyze in a 10% D 2O solution with t 1/2 ranging from 2 to 11 h. The IC 50 values obtained for three of the salen complexes studied on HT-29 colon and OVCAR-1 ovarian cells demonstrate activity that exceeds those of the known tianium(IV) complexes Cp 2TiCl 2 and (bzac) 2Ti(OiPr) 2 and that of cisplatin, where the most active para-chlorinated complex exhibits activity enhancement relative to cisplatin by 10-fold.",

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AB - Salen-titanium(IV) complexes are introduced as a new family of highly efficient antitumor complexes, being the first cytotoxic titanium(IV) complexes of trans labile ligands, as characterized crystallographically. Four complexes with different aromatic substitutions were analyzed, reveling a meaningful effect of the ligand structure on the complex performance. All complexes exhibit high hydrolytic stability, where the labile OAr ligands hydrolyze in a 10% D 2O solution with t 1/2 ranging from 2 to 11 h. The IC 50 values obtained for three of the salen complexes studied on HT-29 colon and OVCAR-1 ovarian cells demonstrate activity that exceeds those of the known tianium(IV) complexes Cp 2TiCl 2 and (bzac) 2Ti(OiPr) 2 and that of cisplatin, where the most active para-chlorinated complex exhibits activity enhancement relative to cisplatin by 10-fold.

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Trans titanium(IV) complexes of salen ligands exhibit high antitumor activity

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