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Tripodal O-N-O bis-Phenolato Amine Titanium(IV) Complexes Show High In Vitro Anti-Cancer Activity

Abid, Mohammed; Nouch, Ryan; Bradshaw, Tracey D.; Lewis, William; Woodward, Simon

Authors

Mohammed Abid

Ryan Nouch

Tracey D. Bradshaw

William Lewis

Simon Woodward



Abstract

The octahedral titanium(IV) complexes trans,mer‐[Ti{R3N(CH2C6H2‐2‐O‐4‐R2‐6‐R1)2}2] (R1 = Me, OMe, Cl; R2 = Me, OMe, F, Cl; R3 = Me, Et; not all combinations) are synthesised in two steps from simple phenols in 36‐53% overall yield. The highly crystalline (4 X‐ray structures) complexes are active against MCF‐7 (breast) and HCT‐116 (colon) cancer cell lines showing widely varying GI50 values in the range 1‐100 µM depending on R1‐R3. Highest activities are realised when R1 = OMe and R2, R3 = Me (GI50 ~1 µM for MCF‐7 and 2‐3 µM for HCT‐116). These are respectively 8× and 3× times greater than the activities of cisplatin in the same cell lines. These titanium complexes show some significant selectivity for cancer cell lines; up to 7× higher in MCF‐7 compared to non‐cancer (MRC‐5) fibroblast cells. Details of cellular mode of action indicators (cell cycle perturbation, Annexin V, γ‐H2AX, and caspase studies) that point to an apoptosis mode for the most active compound (R1 = OMe and R2, R3 = Me) are also reported.

Journal Article Type Article
Publication Date May 11, 2019
Journal European Journal of Inorganic Chemistry
Print ISSN 1434-1948
Publisher Wiley
Peer Reviewed Peer Reviewed
APA6 Citation Abid, M., Nouch, R., Bradshaw, T. D., Lewis, W., & Woodward, S. (2019). Tripodal O-N-O bis-Phenolato Amine Titanium(IV) Complexes Show High In Vitro Anti-Cancer Activity. European Journal of Inorganic Chemistry, doi:10.1002/ejic.201900510
DOI https://doi.org/10.1002/ejic.201900510
Keywords Inorganic Chemistry
Publisher URL https://onlinelibrary.wiley.com/doi/abs/10.1002/ejic.201900510
Additional Information This is the peer reviewed version of the following article: Abid, M. , Nouch, R. , Bradshaw, T. ., Lewis, W. and Woodward, S. (2019), Tripodal O‐N‐O bis‐Phenolato Amine Titanium(IV) Complexes Show High In Vitro Anti‐Cancer Activity. Eur. J. Inorg. Chem., which has been published in final form at https://doi.org/10.1002/ejic.201900510. This article may be used for non-commercial purposes in accordance with Wiley Terms and Conditions for Use of Self-Archived Versions.

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