Two new PtII and PdII complexes of formula [LMCl2] (M = Pt, Pd) were synthesized and characterized both in solution and solid state. They were obtained using the thio-aza macrocycle 9,18-dimethyl-12,17dithia-9,18,27,28-tetraaaza-29-oxatetracyclo[24.2.1.02,7.020,25]enneicosa-2,4,6,20,22,24,26,281-octaene (L) containing the 2,5-diphenyl [1, 3, 4]oxadiazole as intercalating fragment. MII is coordinated in cis-position by the two S atoms of L. The two crystal structures of [LPtCl2] and [LPdCl2] complexes showed that the MII ion is located outside the macrocyclic cavity. The square planar coordination sphere is fulfilled by two chloride anions in a cisplatin-like arrangement with the chloride leaving groups exposed to the environment. The biological activity of both [LPtCl2] and [LPdCl2], monitored towards a leukemic cellular model (U937), is coherent with their ability to interfere, at different levels, with the DNA structure
PdII and PtII complexes with a thio-aza macrocycle ligand containing an intercalating fragment: Structural and antitumor activity studies / Amatori, Stefano; Ambrosi, Gianluca; Errico Provenzano, Alfredo; Fanelli, Mirco; Formica, Mauro; Fusi, Vieri; Giorgi, Luca; Macedi, Eleonora; Micheloni, Mauro; Paoli, Paola; Rossi, Patrizia. - In: JOURNAL OF INORGANIC BIOCHEMISTRY. - ISSN 0162-0134. - STAMPA. - 162:(2016), pp. 154-161. [10.1016/j.jinorgbio.2016.06.027]
PdII and PtII complexes with a thio-aza macrocycle ligand containing an intercalating fragment: Structural and antitumor activity studies
MACEDI, ELEONORA;PAOLI, PAOLA;ROSSI, PATRIZIA
2016
Abstract
Two new PtII and PdII complexes of formula [LMCl2] (M = Pt, Pd) were synthesized and characterized both in solution and solid state. They were obtained using the thio-aza macrocycle 9,18-dimethyl-12,17dithia-9,18,27,28-tetraaaza-29-oxatetracyclo[24.2.1.02,7.020,25]enneicosa-2,4,6,20,22,24,26,281-octaene (L) containing the 2,5-diphenyl [1, 3, 4]oxadiazole as intercalating fragment. MII is coordinated in cis-position by the two S atoms of L. The two crystal structures of [LPtCl2] and [LPdCl2] complexes showed that the MII ion is located outside the macrocyclic cavity. The square planar coordination sphere is fulfilled by two chloride anions in a cisplatin-like arrangement with the chloride leaving groups exposed to the environment. The biological activity of both [LPtCl2] and [LPdCl2], monitored towards a leukemic cellular model (U937), is coherent with their ability to interfere, at different levels, with the DNA structureFile | Dimensione | Formato | |
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