The Pt(IV) diazido complex trans,trans,trans-[Pt(N(3))(2)(OH)(2)(pyridine)(2)] (1) is unreactive in the dark but is cytotoxic when photoactivated by UVA and visible light. We have shown that 1 when photoactivated accumulates in tumor cells and binds strongly to nuclear DNA under conditions in which it is toxic to tumor cells. The nature of the DNA adducts, including conformational alterations, ...

This review covers twenty four Pt(II) complexes of the inner coordination sphere Pt(κ3–P1 N1N2)(Y), (Y = Cl, CL); Pt(κ3–P1N1X1)(Y), (X1 O1 and Y P2L, I); C1 NL, Cl); S1 Se1 Pt(κ3–N1P1N2)(Cl), Pt(κ3–S1P1S2)(Cl), Pt(κ3–P1S1Cl1)(Cl) Pt(κ3–P1Si1N1)(OL). These are crystallized in three crystal classes: monoclinic (16 examples), triclinic (5 orthorhombic (3 examples). Each κ3–ligand creates two metal...

The human metallo-chaperone protein Atox1 features a high affinity Cu(I) binding site Cys(12)GlyGlyCys(15) (KD = 10(-17.4) M at pH 7.0) and delivers copper to the trans-Golgi network (TGN). Atox1 may participate in the metabolism of the drug cis-Pt(NH3)2Cl2 (cisplatin), either as a component of its delivery to the nucleus or of its loss via transport to the TGN and beyond. The species of stoich...

This study examines the mechanisms by which thioumeamay protect cells against toxic actions produced by platinum com plexes or nitrogen mustards. Mouse leukemia Li 210 cells were assayed for survival by colony formation in soft agamand for DNA interstrand cross-linking using the alkaline elution method. The survival of Li 2i 0 cells treated with cis-and trans Pt(Il)diamminedichloride was enhanc...

The use of Pt(IV) complexes as pro-drugs that are activated by intracellular reduction is a widely investigated approach to overcome the limitations of Pt(II) anticancer agents. A series of ten mono- and bis-carboxylated Pt(IV) complexes with axial indole-3-acetic acid (IAA) and indole-3-propionic acid (IPA) ligands were synthesized and characterized by elemental analysis, ESI-MS, FT-IR, (1)H a...

A rhodamine moiety was used for the preparation of trans bis(tributylphosphine) Pt(II) bisacetylide complexes (RH-BDPY-Pt-1 and RH-BDPY-Pt-2, with two different Bodipy acetylide ligands), which show acid/base-switchable photophysical properties. The rhodamine moiety undergoes reversible spirolactam ↔ opened amide structure transformation in the presence of an acid/base. Bodipy ligands are respo...

Oxidation of the acetate-bridged half-lantern platinum(II) complex cis-[Pt(II)(NH(3))(2)(μ-OAc)(2)Pt(II)(NH(3))(2)](NO(3))(2), [1](NO(3))(2), with iodobenzene dichloride or bromine generates the halide-capped platinum(III) species cis-[XPt(III)(NH(3))(2)(μ-OAc)(2)Pt(III)(NH(3))(2)X](NO(3))(2), where X is Cl in [2](NO(3))(2) or Br in [3](NO(3))(2), respectively. These three complexes, characteri...

The substitution of aqua ligands of mononuclear Pt(II) complexes of the general form [Pt(H(2)O)(N,N-bis(2-pyridylmethyl)-N(CH(2))(n)-CH(3); -NC(CH(3))(3); -NH](CF(3)SO(3))(2), n = 1 (bpea); 2 (bppa); 3 (bpba); 5 (bpha), 9 (bpda) -NC(CH(3))(3) (bpbta) and -NH (bpma) by thiourea nucleophiles was investigated under pseudo first-order conditions as a function of concentration and temperature using ...