A novel cytotoxic ternary copper(II) complex of 1,10-phenanthroline and L-threonine with DNA nuclease activity.
A novel ternary copper(II) complex, [Cu(phen)(L-Thr)(H2O)](ClO4) (phen=1,10-phenanthroline, L-Thr=L-threonine), has been synthesized and structurally characterized. The complex crystallized in a triclinic system with space group P1 , a=7.526(15) A, b=11.651(2) A, c=12.127(2) A, alpha=115.41(3) degrees , beta=102.34(3) degrees and gamma=91.33(3) degrees . The copper(II) center is situated in a distorted square-pyramidal geometry. At a concentration of 10(-6) mol L(-1), the complex exhibited potent cytotoxic effects against human leukemia cell line HL-60 and human stomach cancer cell line SGC-7901 with inhibition rates of over 90%, however, less pronounced effects were observed for human liver carcinoma cell line BEL-7402 and human non-small-cell lung cancer cell line A-549. The complex was shown to bind DNA by intercalation and cleave pBR322 DNA in the presence of ascorbate.
Zhang
Shouchun
S
State Key Laboratory of Coordination Chemistry, Coordination Chemistry Institute, Nanjing University, Nanjing 210093, PR China.
Zhu
Yangguang
Y
Tu
Chao
C
Wei
Haiying
H
Yang
Zhen
Z
Lin
Liping
L
Ding
Jian
J
Zhang
Junfeng
J
Guo
Zijian
Z
D001205:Ascorbic Acid / Q000378:metabolism; D045744:Cell Line, Tumor; D002942:Circular Dichroism; D003300:Copper / Q000737:chemistry* / Q000378:metabolism; D018360:Crystallography, X-Ray; D004278:DNA, Superhelical / Q000737:chemistry / Q000378:metabolism*; D003851:Deoxyribonucleases / Q000737:chemistry* / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D006131:Growth Inhibitors / Q000378:metabolism / Q000494:pharmacology; D018922:HL-60 Cells; D006801:Humans; D007364:Intercalating Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism*; D008968:Molecular Conformation; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism / Q000633:toxicity*; D010618:Phenanthrolines / Q000737:chemistry; D013050:Spectrometry, Fluorescence; D013056:Spectrophotometry, Ultraviolet; D013912:Threonine / Q000737:chemistry* / Q000378:metabolism; D014867:Water / Q000737:chemistry
D004278:DNA, Superhelical; D006131:Growth Inhibitors; D007364:Intercalating Agents; D009942:Organometallic Compounds; D010618:Phenanthrolines; D014867:Water; D013912:Threonine; D003300:Copper; D003851:Deoxyribonucleases; D001205:Ascorbic Acid