title: [Zn(phen)(O,N,O)(H2O)] and [Zn(phen)(O,N)(H2O)] with O,N,O is 2,6-dipicolinate and N,O is L-threoninate: synthesis, characterization, and biomedical properties.
abstract: Two ternary Zn(II) complexes, with 1,10-phenanthroline (phen) as the main ligand and a carboxylate-containing ligand [dipicolinate (dipico) or L-threoninate (L-Thr)] as the subsidiary ligand, were prepared and characterized by elemental analysis, Fourier transform IR, UV, and fluorescence spectroscopy, X-ray diffraction, molar conductivity, and electrospray ionization mass spectrometry. X-ray structure analysis shows that both [Zn(phen)(dipico)(H(2)O)]·H(2)O (1) and [Zn(phen)(L-Thr)(H(2)O)Cl]·2H(2)O (2) have octahedral geometry about the Zn(II) atom. Both complexes can inhibit topoisomerase I, and have better anticancer activity than cisplatin against nasopharyngeal cancer cell lines, HK1 and HONE-1, with concentrations causing 50 % inhibition of cell proliferation (IC(50)) in the low micromolar range. Complex 2 has the highest therapeutic index for HK1. Both Zn(II) complexes can induce cell death by apoptosis. Changing the subsidiary ligand in the Zn(II) complexes affects the UV-fluorescence spectral properties of the coordinated phen ligand, the binding affinity for some DNA sequences, nucleobase sequence-selective binding, the phase at which cell cycle progression was arrested for treated cancer cells, and their therapeutic index.
authors: Faculty of Science, Universiti Tunku Abdul Rahman, 3190, Kampar, Malaysia.
authors: Lee-Fang
authors: LF
authors: Chin
authors: Siew-Ming
authors: SM
authors: Kong
authors: Hoi-Ling
authors: HL
authors: Seng
authors: Yee-Lian
authors: YL
authors: Tiong
authors: Kian-Eang
authors: KE
authors: Neo
authors: Mohd Jamil
authors: MJ
authors: Maah
authors: Alan Soo-Beng
authors: AS
authors: Khoo
authors: Munirah
authors: M
authors: Ahmad
authors: Tzi-Sum Andy
authors: TS
authors: Hor
authors: Hong-Boon
authors: HB
authors: Lee
authors: Swee-Lan
authors: SL
authors: San
authors: Soi-Moi
authors: SM
authors: Chye
authors: Chew-Hee
authors: CH
authors: Ng
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002945:Cisplatin / Q000737:chemistry / Q000494:pharmacology; D056831:Coordination Complexes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D018360:Crystallography, X-Ray; D006801:Humans; D020128:Inhibitory Concentration 50; D008958:Models, Molecular; D015394:Molecular Structure; D010618:Phenanthrolines / Q000737:chemistry* / Q000494:pharmacology; D011725:Pyridines / Q000737:chemistry*; D017550:Spectroscopy, Fourier Transform Infrared; D013912:Threonine / Q000737:chemistry*; D059003:Topoisomerase Inhibitors / Q000737:chemistry / Q000494:pharmacology; D015032:Zinc / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D056831:Coordination Complexes; D010618:Phenanthrolines; D011725:Pyridines; D059003:Topoisomerase Inhibitors; C048697:2,3,4,5-tetrahydro-2,6-pyridinedicarboxylic acid; D013912:Threonine; D015032:Zinc; D002945:Cisplatin; C025205:1,10-phenanthroline