Cyclometalated gold(III) complexes with N-heterocyclic carbene ligands as topoisomerase I poisons

Jessie Jing Yan; Andy Lok-Fung Chow; Chung-Hang Leung; Raymond Wai-Yin Sun; Dik-Lung Ma; Chi-Ming Che

doi:10.1039/c001216e

Cyclometalated gold(III) complexes with N-heterocyclic carbene ligands as topoisomerase I poisons

Chem Commun (Camb). 2010 Jun 14;46(22):3893-5. doi: 10.1039/c001216e. Epub 2010 Apr 19.

Authors

Jessie Jing Yan¹, Andy Lok-Fung Chow, Chung-Hang Leung, Raymond Wai-Yin Sun, Dik-Lung Ma, Chi-Ming Che

Affiliation

¹ 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.

PMID: 20401423
DOI: 10.1039/c001216e

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Antineoplastic Agents / chemistry*
Antineoplastic Agents / therapeutic use
Antineoplastic Agents / toxicity
Carcinoma, Hepatocellular / drug therapy
Computer Simulation
Coordination Complexes / chemistry*
Coordination Complexes / therapeutic use
Coordination Complexes / toxicity
DNA Topoisomerases, Type I / metabolism
Gold / chemistry*
Hep G2 Cells
Heterocyclic Compounds / chemistry*
Humans
Ligands
Liver Neoplasms / drug therapy
Methane / analogs & derivatives*
Methane / chemistry
Mice
Mice, Nude
Topoisomerase I Inhibitors*

Substances

Antineoplastic Agents
Coordination Complexes
Heterocyclic Compounds
Ligands
Topoisomerase I Inhibitors
carbene
Gold
DNA Topoisomerases, Type I
Methane