L-Carnitine, a biomolecule able to cross the blood-brain barrier exploiting specific transporters, behaves as mono or bidentate anionic ligand for Pt(II) in the new amino complexes cis-[Pt(L-carnitine-O)2(NH3)2](BF4)2 (1), cis-[PtCl(L-carnitina-O)(NH3)2]BF4 (2), [Pt(L-carnitine-O,O’)(1,2-DACH)]BF4 (3), [Pt(L-carnitine-O)2(1,2-DACH)](BF4)2 (4), and [PtCl(L-carnitine-O)(1,2-DACH)](BF4) (5). Four complexes with DMSO have been also prepared and characterized: the synthetic intermediate [Pt(CO3)(DMSO)2] (6), [Pt(L-carnitine-O,O’)(DMSO)2]BF4 (7), cis-[Pt(L-carnitine-O)2(DMSO)2](BF4)2 (8) and cis-[PtCl(L-carnitine-O)(DMSO)2]BF4, (9). The antiproliferative activity of three representative complexes 1, 5 and 7 has been assayed against three human cancer cell lines A2780, K562 and SKOV3, and it was found comparable to that of the parent active compounds cis-[PtCl2(1,2-DACH)] and cisplatin.
Synthesis, characterization and antiproliferative activity of amino- and DMSO complexes of platinum(II) containing L-carnitine
BERGAMINI, Paola
Primo
;MARVELLI, LorenzaSecondo
;SPIRANDELLI, GIULIAPenultimo
;GALLERANI, EleonoraUltimo
2016
Abstract
L-Carnitine, a biomolecule able to cross the blood-brain barrier exploiting specific transporters, behaves as mono or bidentate anionic ligand for Pt(II) in the new amino complexes cis-[Pt(L-carnitine-O)2(NH3)2](BF4)2 (1), cis-[PtCl(L-carnitina-O)(NH3)2]BF4 (2), [Pt(L-carnitine-O,O’)(1,2-DACH)]BF4 (3), [Pt(L-carnitine-O)2(1,2-DACH)](BF4)2 (4), and [PtCl(L-carnitine-O)(1,2-DACH)](BF4) (5). Four complexes with DMSO have been also prepared and characterized: the synthetic intermediate [Pt(CO3)(DMSO)2] (6), [Pt(L-carnitine-O,O’)(DMSO)2]BF4 (7), cis-[Pt(L-carnitine-O)2(DMSO)2](BF4)2 (8) and cis-[PtCl(L-carnitine-O)(DMSO)2]BF4, (9). The antiproliferative activity of three representative complexes 1, 5 and 7 has been assayed against three human cancer cell lines A2780, K562 and SKOV3, and it was found comparable to that of the parent active compounds cis-[PtCl2(1,2-DACH)] and cisplatin.File | Dimensione | Formato | |
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