Synthesis, characterization and biological activity of complexes of lanthanum(Ⅲ) with 2-(1'-phenyl- 2'-carboxyl-3'-aza-n-butyl)- 1,10-phenanthroline and 2-(1'-p-phenol-2'-carboxyl-3'-aza-n-butyl)- 1,10-phenanthroline

摘要

Two novel ligands 2-(1'-phenyl-2'-carboxyl-3'-aza-n-butyl)-1,10-phenanthroline (L1) and 2-(1'-p-phenol-2'-carboxyl-3'-aza-butyl)-1,10-phenanthroline (L2), and their La(Ⅲ) complexes of La(Ⅲ)L1, La(Ⅲ)(L1)_2, La(Ⅲ)L2, and La(Ⅲ)(L2)_2, were synthesized and characterized by ~1H NMR, elemental analysis, IR, thermal analysis and conductance measurement. All complexes have been assayed for anticancer activity in vitro against HL-60 (human leukocytoma) cells, PC-3MIE8 (human prostate carcinoma) cells, BGC-823 (human stomach carcinoma) cells, MDA-MB-435 (human galactophore carcinoma) cells, Bel-7402 (human liver carcinoma) cells, and HeLa (human cervix carcinoma) cells. Results showed that the two complexes La(Ⅲ)L1 and La(Ⅲ)(L1)_2 exhibited good cytotoxic activity against different cell lines in general; and La(Ⅲ)(L1)_2 is more effective than cisplatin against all six cell lines. DNA-binding studies indicated that, besides the intercalation, the complexes bind to DNA by the other interaction(s).