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 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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