1,720,976 research outputs found
Activation of antitumoral platinum prodrugs for the local treatment of bone tumors by inclusion in bioactive inorganic matrices.
No full textPlatinum-containing bisphosphonate complexes as potentially targeted chemotherapeutics for malignant mesothelioma.
No full textBioactive Inorganic Matrices for the Local Delivery of Platinum-based Prodrugs in the Treatment of Bone Tumors
No full textDinuclear Pt(ii)-bisphosphonate complexes: A scaffold for multinuclear or different oxidation state platinum drugs
No full textGeminal bisphosphonates (BPs), used in the clinic for the treatment of hypercalcaemia and skeletal metastases, have been also exploited for promoting the specific accumulation of platinum antitumor drugs in bone tissue. In this work, the platinum dinuclear complex [{Pt(en)}2(μ-AHBP-H 2)]+ (1) (the carbon atom bridging the two phosphorous atoms carrying a 2-ammonioethyl and a hydroxyl group, AHBP-H2) has been used as scaffold for the synthesis of a Pt(ii) trinuclear complex, [{Pt(en)}3(μ-AHBP)]+ (2), and a Pt(iv) adamantane-shaped dinuclear complex featuring an oxo-bridge, [{Pt IV(en)Cl}2(μ-O)(μ-AHBP-H2)]+ (3) (X-ray structure). Compound 2 undergoes a reversible, pH dependent, rearrangement with a neat switch point around pH = 5.4. Compound 3 undergoes a one-step electrochemical reduction at Epc = -0.84 V affording compound 1. Such a potential is far lower than that of glutathione (-0.24 V), nevertheless compound 3 can undergo chemical reduction to 1 by GSH, most probably through a different (inner-sphere) mechanism. In vitro cytotoxicity of the new compounds, tested against murine glioma (C6) and human cervix (HeLa) and hepatoma (HepG2) cell lines, has shown that, while the PtIV dimer 3 is inactive up to a concentration of 50 μM, the two PtII polynuclear compounds 1 and 2 have a cytotoxicity comparable to that of cisplatin with the trinuclear complex 2 generally more active than the dinuclear complex 1. © 2012 The Royal Society of Chemistry
Synthesis, characterization, and cytotoxicity of platinum-bisphosphonate complexes to be used as prodrugs in the local treatment of bone tumors.
No full textA model radiopharmaceutical agent targeted to translocator protein 18 kDa (TSPO)
No full textA stable Re complex containing an imidazopyridine ligand with a
high affinity for TSPO has been synthesized as a model for new
99mTc or 188/186Re-based radiopharmaceuticals to be used in
SPECT diagnosis or in therapy, respectively. The new complex fac-
[ReBr(CO)3(TZ6)], structurally characterized, showed high affinity
(nanomolar concentration) for the target protein
Dinuclear Pt(II)-bisphosphonate complexes:useful building blocks for the preparation of multinuclear or higher oxidation state platinum drugs.
No full textDesign, characterization, and in vitro affinity of new Pt coordination compounds containing TSPO ligands
No full textDinuclear Pt(II)-bisphosphonate complexes: a scaffold for multinuclear or different oxidation state platinum drugs.
No full textGeminal bisphosphonates (BPs), used in the clinic for the treatment of hypercalcaemia and skeletal metastases, have been also exploited for promoting the specific accumulation of platinum antitumor drugs in bone tissue. In this work, the platinum dinuclear complex [{Pt(en)}2(μ-AHBP-H2)]+ (1) (the carbon atom bridging the two phosphorous atoms carrying a 2-ammonioethyl and a hydroxyl group, AHBP-H2) has been used as scaffold for the synthesis of a Pt(II) trinuclear complex, [{Pt(en)}3(μ-AHBP)]+ (2), and a Pt(IV) adamantane-shaped dinuclear complex featuring an oxo-bridge, [{PtIV(en)Cl}2(μ-O)(μ-AHBP-H2)]+ (3) (X-ray structure). Compound 2 undergoes a reversible, pH dependent, rearrangement with a neat switch point around pH = 5.4. Compound 3 undergoes a one-step electrochemical reduction at Epc = −0.84 V affording compound 1. Such a potential is far lower than that of glutathione (−0.24 V), nevertheless compound 3 can undergo chemical reduction to 1 by GSH, most probably through a different (inner-sphere) mechanism. In vitro cytotoxicity of the new compounds, tested against murine glioma (C6) and human cervix (HeLa) and hepatoma (HepG2) cell lines, has shown that, while the PtIV dimer 3 is inactive up to a concentration of 50 μM, the two PtII polynuclear compounds 1 and 2 have a cytotoxicity comparable to that of cisplatin with the trinuclear complex 2 generally more active than the dinuclear complex 1
Dinuclear platinum(II)-bisphosphonate complexes as potentially targeted chemotherapeutics for malignant mesothelioma.
No full text- …
