| Literature DB >> 20822096 |
Frédéric Pelletier1, Virginie Comte, Alexandre Massard, Margot Wenzel, Stéphanie Toulot, Philippe Richard, Michel Picquet, Pierre Le Gendre, Olivier Zava, Fabio Edafe, Angela Casini, Paul J Dyson.
Abstract
A series of bimetallic titanium-ruthenium complexes of general formula [(η(5)-C(5)H(5))(μ-η(5):κ(1)-C(5)H(4)(CR(2))(n)PR'R'')TiCl(2)](η(6)-p-cymene)RuCl(2) (n = 0, 1, 2 or 4; R = H or Me; R' = H, Ph, or Cy; R'' = Ph or Cy) have been synthesized, including two novel compounds as well as two cationic derivatives of formula [(η(5)-C(5)H(5))(μ-η(5):κ(1)-C(5)H(4)(CH(2))(n)PPh(2))TiCl(2)] [(η(6)-p-cymene)RuCl](BF(4)) (n = 0 or 2). The solid state structure of two of these compounds was also established by X-ray crystallography. The complexes showed a cytotoxic effect on human ovarian cancer cells and were markedly more active than their Ti or Ru monometallic analogues titanocene dichloride and RAPTA-C, respectively. Studies of cathepsin B inhibition, an enzyme involved in cancer progression, showed that enzyme inhibition by the bimetallic complexes is influenced by the length of the alkyl chain in between the metal centers. Complementary ESI-MS studies provided evidence for binding of a Ru(II) fragment to proteins.Entities:
Mesh：
Substances：
Year: 2010 PMID： 20822096 DOI： 10.1021/jm1004804
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446