European Journal of Inorganic Chemistry p. 2774 - 2780 (2019)
Update date:2022-08-10
Topics:
Abid, Mohammed
Nouch, Ryan
Bradshaw, Tracey D.
Lewis, William
Woodward, Simon
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 ca. 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.||||||.
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