Cyclometalated gold(III) complexes with N-heterocyclic carbene ligands as topoisomerase I poisons.
A panel of stable [Au(R-C--N--C)(N-heterocyclic carbene)](+) complexes displays prominent in vitro anticancer properties; [Au(C--N--C)(IMe)]CF(3)SO(3) (1, IMe = 1,3-dimethylimidazol-2-ylidene) significantly poisons topoisomerase I in vitro and suppresses tumor growth in nude mice model.
Yan
Jessie Jing
JJ
Department of Chemistry and Open Laboratory of Chemical Biology of the Institute of Molecular Technology for Drug Discovery and Synthesis, The University of Hong Kong, Pokfulam Road, Hong Kong, China.
Chow
Andy Lok-Fung
AL
Leung
Chung-Hang
CH
Sun
Raymond Wai-Yin
RW
Ma
Dik-Lung
DL
Che
Chi-Ming
CM
D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000627:therapeutic use / Q000633:toxicity; D006528:Carcinoma, Hepatocellular / Q000188:drug therapy; D003198:Computer Simulation; D056831:Coordination Complexes / Q000737:chemistry* / Q000627:therapeutic use / Q000633:toxicity; D004264:DNA Topoisomerases, Type I / Q000378:metabolism; D006046:Gold / Q000737:chemistry*; D056945:Hep G2 Cells; D006571:Heterocyclic Compounds / Q000737:chemistry*; D006801:Humans; D008024:Ligands; D008113:Liver Neoplasms / Q000188:drug therapy; D008697:Methane / Q000031:analogs & derivatives* / Q000737:chemistry; D051379:Mice; D008819:Mice, Nude; D059004:Topoisomerase I Inhibitors
D000970:Antineoplastic Agents; D056831:Coordination Complexes; D006571:Heterocyclic Compounds; D008024:Ligands; D059004:Topoisomerase I Inhibitors; C030011:carbene; D006046:Gold; D004264:DNA Topoisomerases, Type I; D008697:Methane