In this work was to evaluate the cytotoxic activity of a series of monomeric group 3 and lanthanide (N,​N,​N)​-​heteroscorpionate-​triflate complexes (M (OTf) 2 (cybpamd) (THF)​) (Ln = Sc (2)​, Y (3)​, La (4)​, Nd (5)​, Sm (6)​, Dy (7)​, Yb (8)​; OTf = SO3CF3; cybpamd = N, N'-​dicyclohexyl-​2,​2-​bis-​(3,​5-​dimethyl-​pyrazol-​1-​yl)​-​acetamidinate) having octahedral geometry around the metal atoms on the human epithelial lung adenocarcinoma (A549)​, human melanoma (A375)​, human cervical epithelial adenocarcinoma, human embryonic kidney (HEK-​293) and murine macrophages (J774.A1) cell lines. Methods All the tested compds. were incubated with cells for 72 h and their growth inhibition assessed by using MTT assay. Key findings On the cell line HEK-​293 complexes 5 and 7 show a reasonable activities, while the murine macrophage cell line (J774.A1)​, only the scandium 2 complex is not very active. All complexes tested are poorly active on human health adenocarcinoma lung epithelial (A549) and human melanoma (A375)​. Conclusions The group 3 and lanthanide (N,​N,​N)​-​heteroscorpionate triflate-​complexes (M(OTf)​2(cybpamd)​(THF)​) on murine macrophage (J774.A1) cell line, except that of scandium, show a reasonable activity. On human epithelial cervix adenocarcinoma (HeLa) complexes 3, 5 and 6 are significantly more active than cis-​platinum, as well as complex 5 is more active on human embryonic kidney (HEK-​293) cell line. All the tested complexes are poorly active on human epithelial lung adenocarcinoma (A549) and human melanoma (A375)​. The different behavior of the complexes examd. (2-​8) let us hypothesize that the cytotoxic activity is related to the mol. as a whole and not only to the ligand or the metal ion sep.

New insights on cytotoxic activity of group 3 and lanthanide compounds: complexes with [N,N,N]-scorpionate ligands

SATURNINO, Carmela;NAPOLI, Mariagrazia;POPOLO, Ada;PINTO, Aldo;LONGO, Pasquale;
2013-01-01

Abstract

In this work was to evaluate the cytotoxic activity of a series of monomeric group 3 and lanthanide (N,​N,​N)​-​heteroscorpionate-​triflate complexes (M (OTf) 2 (cybpamd) (THF)​) (Ln = Sc (2)​, Y (3)​, La (4)​, Nd (5)​, Sm (6)​, Dy (7)​, Yb (8)​; OTf = SO3CF3; cybpamd = N, N'-​dicyclohexyl-​2,​2-​bis-​(3,​5-​dimethyl-​pyrazol-​1-​yl)​-​acetamidinate) having octahedral geometry around the metal atoms on the human epithelial lung adenocarcinoma (A549)​, human melanoma (A375)​, human cervical epithelial adenocarcinoma, human embryonic kidney (HEK-​293) and murine macrophages (J774.A1) cell lines. Methods All the tested compds. were incubated with cells for 72 h and their growth inhibition assessed by using MTT assay. Key findings On the cell line HEK-​293 complexes 5 and 7 show a reasonable activities, while the murine macrophage cell line (J774.A1)​, only the scandium 2 complex is not very active. All complexes tested are poorly active on human health adenocarcinoma lung epithelial (A549) and human melanoma (A375)​. Conclusions The group 3 and lanthanide (N,​N,​N)​-​heteroscorpionate triflate-​complexes (M(OTf)​2(cybpamd)​(THF)​) on murine macrophage (J774.A1) cell line, except that of scandium, show a reasonable activity. On human epithelial cervix adenocarcinoma (HeLa) complexes 3, 5 and 6 are significantly more active than cis-​platinum, as well as complex 5 is more active on human embryonic kidney (HEK-​293) cell line. All the tested complexes are poorly active on human epithelial lung adenocarcinoma (A549) and human melanoma (A375)​. The different behavior of the complexes examd. (2-​8) let us hypothesize that the cytotoxic activity is related to the mol. as a whole and not only to the ligand or the metal ion sep.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11386/4170453
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