Gold(I) bis(N‐heterocyclic carbene) complexes: Metabolic stability,in vitro inhibition,and genotoxicity |
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| Authors: | Jackie Tan Haresh Sivaram Han Vinh Huynh |
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| Affiliation: | Department of Chemistry, National University of Singapore, Singapore |
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| Abstract: | We report the profiling of the metabolic stability, normal cell inhibition, and genotoxicity of the two gold complexes Au (iPr2‐bimy)2]PF6 ( 1 ) and Au (Fpyr)(iPr2‐bimy)]PF6 ( 2 ), which show strong apoptotic activities in lung cancer cells. Liver microsomal tests revealed that the compounds have a relatively high half‐life compared to midazolam and do not suffer rapid metabolism and in vitro clearance. The cytotoxic potential of these compounds were also relatively weak in normal cells, with higher IC50 values compared to cancer cells, with a 2–60 times difference. The Ames test revealed that the compounds do not give rise to any mutations as well. Overall, the compounds showed stability in liver microsomes, specificity for cancer cells, and a lack of genotoxic potential. |
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| Keywords: | Gold N‐heterocyclic carbene Anti‐proliferative activity Mutagenicity Lipophilicity Metabolic stability |
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