title: Inhibition of mitogen-activated protein kinase (MAPK) and cyclin-dependent kinase 2 (Cdk2) by platinum(II) phenanthroline complexes.
abstract: Inhibition of protein kinases in the fight against disease remains a constant challenge for medicinal chemists, who have screened multitudes of predominantly planar organic scaffolds, natural and synthetic, to identify potent-albeit not always selective-kinase inhibitors. Herein, in an effort to investigate the potential biological utility of metal-based compounds as inhibitors against the cancer-relevant targets mitogen-activated protein kinase and cyclin-dependent kinase 2, we explore various parameters in planar platinum(II) complexes with substituted phenanthroline ligands and aliphatic diamine chelate co-ligands, to identify combinations that yield promising inhibitory activity. The individual ligands' steric requirements as well as their pattern of hydrogen bond donors/acceptors appear to alter inhibitory potency when modulated.
  
  
  BACKGROUND
  The online version of this article (doi:10.1007/s12154-011-0059-5) contains supplementary material, which is available to authorized users.
authors.forename: Emma S
authors.initials: ES
authors.lastname: Child
authors.forename: Savvas N
authors.initials: SN
authors.lastname: Georgiades
authors.forename: Kirsten N
authors.initials: KN
authors.lastname: Rose
authors.forename: Verity S
authors.initials: VS
authors.lastname: Stafford
authors.forename: Chirag B K
authors.initials: CB
authors.lastname: Patel
authors.forename: Joachim H G
authors.initials: JH
authors.lastname: Steinke
authors.forename: David J
authors.initials: DJ
authors.lastname: Mann
authors.forename: Ramon
authors.initials: R
authors.lastname: Vilar