Concetta Pacifico

Steric constraints and addition reactions in platinum(II) complexes containing 2,9-dimethyl-1,10-phenanthroline (Me2-phen). X-ray crystal structures of [PtBr2(Me2-phen)] and [PtI2(Me2-phen)]

Abstract [PtX 2 (Me 2 -phen)] complexes (X  Cl ( 1 ), Br ( 2 ), I ( 3 ); Me 2 -phen=2,9-dimethyl1,10-penanthroline) react with dimethylsulfoxide, dimethylsulfide and nitrosobenzene to give the addition products [PtX 2 (Me 2 -phen)(L)] (L  DMS, 1–3a ; DMSO, 1–3b ; PhNO, 1–3c ) containing mono-coordinated Me 2 -phen. The equilibrium constants for the addition reactions ( K f ) have been determined by 1 H NMR spectroscopy and found to be strongly dependent upon the bulkiness of the halogen atoms; log K f increases linearly with the van der Waals radius of the halogens. The crystal structures of the complexes [PtBr 2 (Me 2 -phen ( 2 ) and [PtI 2 (Me 2 -phen)] ( 3 ) have been determined by X-ray diffraction methods. Crystal data for 2 : monoclinic, space group P 2 1 / n , a = 12.155(4), b = 7.933(2), c = 14.522(2) A , β = 93.74(2)°, Z = 4, R = 0.046 . Crystal data for 3 : monoclinic, space group P 2 1 / n , a = 12.542(2), b = 7.957(1), c = 14.976(3) A , β = 94.49(3)°, Z = 4, R = 0.036 . The distortions in the square-planar coordination geometry are compared to those found for the analogous chloro species and correlated to differences in reactivity.

Novel antitumor cisplatin and transplatin derivatives containing 1-methyl-7-azaindole: synthesis, characterization, and cellular responses.

The current work investigates the effect of new bifunctional and mononuclear Pt(II) compounds, the cis- and trans-isomers of [PtCl2(NH3)(L)] (L = 1-methyl-7-azaindole, compounds 1 and 2, respectively), on growth and viability of human carcinoma cells as well as their putative mechanism(s) of cytotoxicity. The results show that substitution of 1-methyl-7-azaindole for ammine in cisplatin or transplatin results in an increase of the toxic efficiency, selectivity for tumor cells in cisplatin-resistant cancer cells, and activation of the trans geometry. The differences in the cytotoxic activities of 1 and 2 were suggested to be due to their different DNA binding mode, different capability to induce cell cycle perturbations, and fundamentally different role of transcription factor p53 in their mechanism of action. Interestingly, both isomers make it possible to detect their cellular uptake and distribution in living cells by confocal microscopy without their modification with an optically active tag.

Platinum complexes with imino ethers or cyclic ligands mimicking imino ethers: synthesis, in vitro antitumour activity, and DNA interaction properties

Both trans- and cis-[PtCl2(NH3)(L)] compounds have been synthesized, L representing either the imino ether HN=C(OMe)Me having a Z or E configuration at the C=N double bond, or the cyclic ligands % MathType!Translator!2!1!AMS LaTeX.tdl!TeX -- AMS-LaTeX! % MathType!MTEF!2!1!+- % feaafeart1ev1aaatCvAUfeBSn0BKvguHDwzZbqefeKCPfgBGuLBPn % 2BKvginnfarmWu51MyVXgatuuDJXwAK1uy0HwmaeHbfv3ySLgzG0uy % 0Hgip5wzaebbnrfifHhDYfgasaacH8YjY-vipgYlH8Gipec8Eeeu0x % Xdbba9frFj0-OqFfea0dXdd9vqai-hGuQ8kuc9pgc9q8qqaq-dir-f % 0-yqaiVgFr0xfr-xfr-xb9adbaqaaeGaciGaaiaabeqaamaabmabaa % GcbaWaaKraaeaacaqGobGaaeypaiaaboeacaqGOaGaae4taiaab2ea % caqGLbGaaeykaiaaboeacaqGibWaaSbaaSqaaiaabkdaaeqaaOGaae % 4qaiaabIeadaWgaaWcbaGaaeOmaaqabaGccaqGdbaaleaaaOGaayzd % SdGaaeisamaaBaaaleaacaqGYaaabeaaaaa!47FE!

Dinuclear Pt(II)-bisphosphonate complexes: a scaffold for multinuclear or different oxidation state platinum drugs†

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ISOMERISM OF AMIDES COORDINATED TO PLATINUM - X-RAY CRYSTAL STRUCTURE OF O-BONDED ACETAMIDE IN A PLATINUM(II) COMPLEX

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Novel Antitumor Platinum(II) Conjugates Containing the Nonsteroidal Anti-inflammatory Agent Diclofenac: Synthesis and Dual Mechanisms of Antiproliferative Effects

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