| Literature DB >> 18605719 |
Divya Krishnamurthy1, Mark R Karver, Edoardo Fiorillo, Valeria Orrú, Stephanie M Stanford, Nunzio Bottini, Amy M Barrios.
Abstract
Gold(I) complexes containing N-heterocyclic carbene ligands were synthesized, characterized, and along with the antiarthritic drug, auranofin, tested as inhibitors of the cysteine-dependent protein tyrosine phosphatases, which are implicated in several disease states. These compounds exhibit potencies in the low micromolar range against the enzymes in vitro. At therapeutically relevant concentrations, all compounds inhibit PTP activity in Jurkat T leukemia cells with some selectivity. In addition, the gold-carbene compounds inhibit phosphatase activity in primary mouse thymocytes.Entities:
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Year: 2008 PMID: 18605719 DOI: 10.1021/jm800101w
Source DB: PubMed Journal: J Med Chem ISSN: 0022-2623 Impact factor: 7.446