期刊
JOURNAL OF ORGANOMETALLIC CHEMISTRY
卷 840, 期 -, 页码 30-37出版社
ELSEVIER SCIENCE SA
DOI: 10.1016/j.jorganchem.2017.03.050
关键词
Carbene-gold anticancer drug; Pseudohalides; Thiolates; NCI 60 cancer cell panel
资金
- School of Chemistry (UCD)
- National Cancer Institute at Maryland/USA
The synthesis and biological evaluation of three gold pseudohalides and three gold thiolates, stabilised by the NHC ligand 1,3-dibenzyl-4,5-diphenyl-imidazol-2-ylidene (NHC*), in order to form stable gold(I) complexes is reported. Two separate procedures have been developed for the synthesis; the one for the pseudohalide complexes employs the use of a biphasic medium while the one for the thiolate complexes requires higher temperature for their formation. The gold complexes have been prepared in varying yields (44-81%) from the corresponding NHC*-Au-Cl precursor. One thiolate and two pseudohalide gold complexes were characterized by single crystal X-ray diffraction and showed the expected monomeric nature of all derivatives. All six complexes were submitted to the NCI 60 cancer cell panel for cytotoxicity tests; most of the complexes showed activity in the medium to low micromolar region, while the NHC*Au-SCN derivative was superior exhibiting nanomolar anticancer activity. (C) 2017 Elsevier B.V. All rights reserved.
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