Copper complex of hydroxyl-substituted triazamacrocyclic ligand and its antitumor activity.
The protonation constants and the stability constants for the formation of copper (II) complex of the ligand [1,4,7] Triazecan-9-ol (L) were presented. Antitumor activity of CuL complex was reported. Preliminary pharmacological tests showed that it had antitumor activity against HXO-RB44 and BEL-7402 cell lines in vitro. Nuclei of [CuL]-stimulated BEL-7402 cells clearly exhibited condensation and break down into chromatin clumps typical of apoptosis. Also it exhibited perturbation effects to BEL-7402 cell lines cycle and further studies showed that it could cleave supercoiled DNA (pBR 322) to nicked and linear DNA.
Liang
Feng
F
Department of Chemistry, Wuhan University, Wuhan 430072, PR China. chemoliangf@yahoo.com.cn
Wu
Chengtai
C
Lin
Huakuan
H
Li
Tao
T
Gao
Dongzhao
D
Li
Zhaoyang
Z
Wei
Jun
J
Zheng
Congyi
C
Sun
Mengxiang
M
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D006690:Bisbenzimidazole; D002453:Cell Cycle / Q000187:drug effects; D002460:Cell Line; D004396:Coloring Agents; D003300:Copper / Q000737:chemistry; D004273:DNA, Neoplasm / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D004591:Electrophoresis, Polyacrylamide Gel; D007202:Indicators and Reagents; D008024:Ligands; D009942:Organometallic Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D011199:Potentiometry
D000970:Antineoplastic Agents; D004396:Coloring Agents; D004273:DNA, Neoplasm; D007202:Indicators and Reagents; D008024:Ligands; D009942:Organometallic Compounds; D003300:Copper; D006690:Bisbenzimidazole