tBu2bpy

tBu2bpy-based Pt(IV) complexes (0-35 μM; 24-48 h) potently suppress the proliferation of Jurkat, K562 and MCF-7 cancer cells. C₁ with a chloro leaving group achieves a minimal IC₅₀ of 1.75 μM toward Jurkat cells, while C₂ bearing a bromo leaving group shows a minimal IC₅₀ of 2.06 μM against Jurkat cells.
tBu2bpy-based Pt(IV) complexes trigger apoptosis in K562 cells, and C1 with a chloro leaving group exerts stronger apoptosis-inducing capacity than C2 bearing a bromo leaving group.
tBu2bpy-derived Pt(IV) complexes have intrinsic binding constants of 3.2×10⁴ M^-1 (C₁) and 3.0×10⁴ M^-1 (C₂) toward hsDNA, revealing a mixed binding mode including partial intercalation and mild structural disturbance of hsDNA. These complexes are capable of displacing ethidium bromide from hsDNA, further verifying their partial intercalation into the double helix of DNA.
tBu2bpy-based Pt(IV) complexes form covalent interactions with 5′-GMP and 5′-AMP, and C₂ carrying a bromo leaving group exhibits higher binding affinity toward these purine nucleotides than C₁ with a chloro leaving group.
tBu2bpy-based complex [Pt(4-ethynylbenzo-15-crown-5)₂(tBu₂bpy)] (compound 1) displays 1035-fold and 870-fold enhancement of its ³MLCT [5d(Pt)→π*(tBu₂bpy)] emission upon the addition of Mg(ClO₄)₂ and Zn(ClO₄)₂, respectively; treatment with 20-100 eq Mg(ClO₄)₂ or Zn(ClO₄)₂ blue-shifts its MLCT absorption band from 393 nm to 383 nm.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.