title: Synthesis, structure, and anticancer activity of gallium(III) complexes with asymmetric tridentate ligands: growth inhibition and apoptosis induction of cisplatin-resistant neuroblastoma cells.
abstract: Five gallium(III) complexes described as [Ga(III)(LX)2]ClO4, where (LX)- is the deprotonated form of a series of asymmetric ligands containing pyridine and 4,6-substituted phenol moieties, were synthesized and characterized by spectroscopic and spectrometric methods. Phenol substituents encompass the electron-withdrawing and electron-donating methoxy (1), nitro (2), chloro (3), bromo (4), and iodo (5) groups. Complexes 1 and 3 have had their molecular structure solved by X-ray crystallography and show distinct coordination modes. Complexes 1-5 were tested for growth-inhibition activity on cisplatin-resistant human neuroblastoma cells; those containing halogen substituents on the phenolate rings, i.e., 3-5, showed activity superior to that observed for cisplatin and induced apoptosis of neuroblastoma cells. Nitro-containing 2 suppressed proliferation of the neuroblastoma cells but induced apoptosis less effectively.
authors.affiliation: Department of Chemistry, Wayne State University, 5101 Cass Avenue, Detroit, MI 48202, USA.
authors.forename: Rajendra
authors.initials: R
authors.lastname: Shakya
authors.forename: Fangyu
authors.initials: F
authors.lastname: Peng
authors.forename: Jianguo
authors.initials: J
authors.lastname: Liu
authors.forename: Mary Jane
authors.initials: MJ
authors.lastname: Heeg
authors.forename: Claudio N
authors.initials: CN
authors.lastname: Verani
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects*; D045744:Cell Line, Tumor; D002478:Cells, Cultured; D002945:Cisplatin / Q000494:pharmacology; D019008:Drug Resistance, Neoplasm / Q000502:physiology*; D005708:Gallium / Q000737:chemistry*; D006131:Growth Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D008024:Ligands; D009447:Neuroblastoma / Q000188:drug therapy*
chemical_list: D000970:Antineoplastic Agents; D006131:Growth Inhibitors; D008024:Ligands; D005708:Gallium; D002945:Cisplatin