Gold(I) complex of N,N'-disubstituted cyclic thiourea with in vitro and in vivo anticancer properties-potent tight-binding inhibition of thioredoxin reductase.
Coinage metal complexes of an N,N'-disubstituted cyclic thiourea exert significant cytotoxicities to cancer cells and, in particular, the gold(i) thiourea complex exhibits a potent tight-binding inhibition of the anticancer drug target thioredoxin reductase with an inhibitory constant at nanomolar level.
Yan
Kun
K
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.
Lok
Chun-Nam
CN
Bierla
Katarzyna
K
Che
Chi-Ming
CM
D000970:Antineoplastic Agents / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D045744:Cell Line, Tumor; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D006046:Gold / Q000737:chemistry*; D006801:Humans; D020128:Inhibitory Concentration 50; D009584:Nitrogen / Q000737:chemistry*; D009942:Organometallic Compounds / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*; D011485:Protein Binding; D013880:Thioredoxin-Disulfide Reductase / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D013890:Thiourea / Q000737:chemistry*
D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D009942:Organometallic Compounds; D006046:Gold; D013880:Thioredoxin-Disulfide Reductase; D013890:Thiourea; D009584:Nitrogen