New insights on cytotoxic activity of group 3 and lanthanide compounds: complexes with [N,N,N]-scorpionate ligands.
OBJECTIVE
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 compounds were incubated with cells for 72 h and their growth inhibition assessed by using MTT assay.


RESULTS
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 behaviour of the complexes examined (2-8) let us hypothesize that the cytotoxic activity is related to the molecule as a whole and not only to the ligand or the metal ion separately.
Dipartimento di Scienze Farmaceutiche, Università di Salerno, Fisciano, Italy. saturnino@unisa.it
Carmela
C
Saturnino
Marco
M
Bortoluzzi
Mariagrazia
M
Napoli
Ada
A
Popolo
Aldo
A
Pinto
Pasquale
P
Longo
Gino
G
Paolucci
D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D057809:HEK293 Cells; D006367:HeLa Cells; D006801:Humans; D007477:Ions; D028581:Lanthanoid Series Elements / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D008024:Ligands; D008264:Macrophages / Q000187:drug effects; D051379:Mice; D015394:Molecular Structure; D009369:Neoplasms / Q000188:drug therapy*; D011720:Pyrazoles / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*
D000970:Antineoplastic Agents; D007477:Ions; D028581:Lanthanoid Series Elements; D008024:Ligands; D011720:Pyrazoles
HEK-293; HeLa; J774.A1; cytotoxic activity; metal complexes