15227-42-6Relevant articles and documents
Platinum(iv)-azido monocarboxylato complexes are photocytotoxic under irradiation with visible light
Butler, Jennifer S.,Clarkson, Guy,Farrer, Nicola J.,Habtemariam, Abraha,Romero, Mar?a J.,Romero-Canelón, Isolda,Sadler, Peter J.,Salassa, Luca,Shaili, Evyenia,Woods, Julie A.
supporting information, p. 10593 - 10607 (2021/08/09)
Complexestrans,trans,trans-[Pt(N3)2(OH)(OCOR)(py)2] where py = pyridine and where OCOR = succinate (1); 4-oxo-4-propoxybutanoate (2) andN-methylisatoate (3) have been synthesized by derivation oftrans,trans,trans-[Pt(OH)2(N3)2(py)2] (4) and characterised by NMR and EPR spectroscopy, ESI-MS and X-ray crystallography. Irradiation of1-3with green (517 nm) light initiated photoreduction to Pt(ii) and release of the axial ligands at a 3-fold faster rate than for4. TD-DFT calculations showed dissociative transitions at longer wavelengths for1compared to4. Complexes1and2showed greater photocytotoxicity than4when irradiated with 420 nm light (A2780 cell line IC50values: 2.7 and 3.7 μM) and complex2was particularly active towards the cisplatin-resistant cell line A2780cis (IC503.7 μM). Unlike4, complexes1-3were phototoxic under green light irradiation (517 nm), with minimal toxicity in the dark. A pKa(H2O) of 5.13 for the free carboxylate group was determined for1, corresponding to an overall negative charge during biological experiments, which crucially, did not appear to impede cellular accumulation and photocytotoxicity.
Compound with antitumor activity, and preparation method and application thereof
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Paragraph 0094; 0095; 0096; 0100, (2017/12/28)
The invention provides a compound with antitumor activity, and a preparation method and application thereof, and relates to the technical field of chemical compounding drugs. The compound is of a structure shown as a formula (I) or (II). The stimuli-responsive self-assembly unimolecular compound with the antitumor activity is prepared through condensation reaction between hepatic-targeting water-soluble lactose and a platinum (IV) compound. The compound has the advantages that hepatic-targeting water-soluble lactose molecules are introduced, water-solubility of the platinum (IV) compound is improved, and hydrophilic-lyophobic balance is achieved, so that the self-assembly unimolecular platinum (IV) compound is formed, cytotoxicity of the platinum (IV) compound is reduced, a compounded tetravalence platinum prodrug has amphipathy, and accumulation degree of hepatoma cells can be increased; due to platinum, activation and release of the platinum compound are benefited under the conditions of external photostimulation or intracellular reduction, and accordingly, high antitumor activity is achieved.
Application of microwave-assisted heating to the synthesis of Pt(II) complexes
Gabano, Elisabetta,Gama, Sofia,Mendes, Filipa,Fregonese, Federico,Paulo, António,Ravera, Mauro
, p. 16 - 19 (2015/09/01)
The microwave-assisted synthesis of Pt(II) complexes containing several pyridines (i.e., pyridine L1, 2-picoline L2, 3-picoline L3, 4-picoline L4, 2,2′-bipyridine L5) is reported. For L1-L5, the reaction was successful in about 50% yield with all the ligands except L2. The same method applied to 4,4′-bis(2-morpholinoethoxy)-2,2′-bipyridine (L6, a ligand showing interesting antiproliferative properties because of a high DNA affinity), was unsatisfactory. The corresponding complex cis-[PtCl2(L6)] was obtained only heating at reflux a mixture of [PtCl2(1,5-cyclooctadiene)] and L6 in acetonitrile for 24 h. Antiproliferative activity of [PtCl2(L6)] on four cancer cell lines (ovarian A2780 and its cisplatin-resistant variant A2780cisR, prostate PC3 and breast cancer MDA-MB-231) was compared with that of its ligand and the model complex [PtCl2(L5)]. These studies showed that [PtCl2(L6)] has just marginal activity towards the tested cells if compared with cisplatin.
