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

作者：Saturnino Carmela^*; Bortoluzzi Marco; Napoli Mariagrazia; Popolo Ada; Pinto Aldo; Longo Pasquale; Paolucci Gino

来源：Journal of Pharmacy and Pharmacology, 2013, 65(9): 1354-1359.

DOI：10.1111/jphp.12112

• cytotoxic activity
• HEK-293
• HeLa
• J774
• A1
• metal complexes

Objectives 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. %26lt;br%26gt;Methods All the tested compounds were incubated with cells for 72 h and their growth inhibition assessed by using MTT assay. %26lt;br%26gt;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). %26lt;br%26gt;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). %26lt;br%26gt;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.

• 出版日期2013-9