In:
Angewandte Chemie, Wiley, Vol. 128, No. 39 ( 2016-09-19), p. 12114-12118
Abstract:
Palladium(II) complexes are generally reactive toward substitution/reduction, and their biological applications are seldom explored. A new series of palladium(II) N‐heterocyclic carbene (NHC) complexes that are stable in the presence of biological thiols are reported. A representative complex, [Pd(C^N^N)(N,N′‐nBu 2 NHC)](CF 3 SO 3 ) ( Pd1 d , HC^N^N=6‐phenyl‐2,2′‐bipyridine, N,N′‐nBu 2 NHC=N,N′‐di‐n‐butylimidazolylidene), displays potent killing activity toward cancer cell lines (IC 50 =0.09–0.5 μ m ) but is less cytotoxic toward a normal human fibroblast cell line (CCD‐19Lu, IC 50 =11.8 μ m ). In vivo anticancer studies revealed that Pd1 d significantly inhibited tumor growth in a nude mice model. Proteomics data and in vitro biochemical assays reveal that Pd1 d exerts anticancer effects, including inhibition of an epidermal growth factor receptor pathway, induction of mitochondrial dysfunction, and antiangiogenic activity to endothelial cells.
Type of Medium:
Online Resource
ISSN:
0044-8249
,
1521-3757
DOI:
10.1002/ange.v128.39
DOI:
10.1002/ange.201602814
Language:
English
Publisher:
Wiley
Publication Date:
2016
detail.hit.zdb_id:
506609-8
detail.hit.zdb_id:
1479266-7