Combining the platinum(ii) drug candidate kiteplatin with 1, 10-phenanthroline analogues. Issue 7 (1st December 2017)

• Record Type: Journal Article
• Authors: Pages, Benjamin J.; Sakoff, Jennette; Gilbert, Jayne; Zhang, Yingjie; Kelly, Sharon M.; Hoeschele, James D.; Aldrich-Wright, Janice R.
• Is Part Of: Dalton transactions. Volume 47:Issue 7(2018)
• Page Start: 2156
• Page End: 2163
• Publication Date: 2017-12-01
• Subjects: Chemistry, Inorganic -- Periodicals; Chemistry, Physical and theoretical -- Periodicals; Chemistry, Inorganic -- Periodicals; 546.05
• DOI: 10.1039/c7dt04108j
• Languages: English
• ISSNs: 1477-9226

Abstract

Abstract : Drug candidate kiteplatin has been combined with analogues of 1, 10-phenanthroline, and the DNA affinity and cytotoxicity have been assessed. Abstract : Platinum complexes of the type [Pt(PL )(AL )] 2+ where PL is a derivative of 1, 10-phenanthroline and AL is cis -1, 4-diaminocyclohexane (1, 4-dach), have been synthesised and characterised by ultraviolet spectroscopy, elemental microanalysis, nuclear magnetic resonance and X-ray crystallography. The calf-thymus DNA binding affinity of these complexes was determined by isothermal titration calorimetry, revealing higher DNA affinity than their 1 S, 2 S -diaminocyclohexane analogues. In vitro cytotoxicity was assessed in eleven human cell lines, revealing unexpectedly low activity for the 1, 4-dach complexes.