Royal College of Surgeons in Ireland
Browse
Synthesis and characterisation of a novel mono functionalisable Pt(IV) oxaliplatin-type complex and its peptide conjugate.pdf (520.9 kB)

Synthesis and characterisation of a novel mono functionalisable Pt(IV) oxaliplatin-type complex and its peptide conjugate

Download (520.9 kB)
journal contribution
posted on 2023-07-31, 16:48 authored by Eolann Kitteringham, Aoife Mckeon, Paul O'DowdPaul O'Dowd, Marc DevocelleMarc Devocelle, Brona MurphyBrona Murphy, Darren GriffithDarren Griffith
The synthesis and characterisation of a novel Pt(IV) monocarboxy precursor complex c,c,t-[Pt(DACH)(Ox)(OEt)(Suc)], which can be employed to synthesise mono functionalised Pt(IV) oxaliplatin-based complexes is reported. Reaction of c,c,t-[Pt(DACH)(Ox)(OEt)(Suc)] with a tumour penetrating peptide, TPP, afforded the corresponding novel monofunctionalised Pt(IV) peptide conjugate c,c,t-[Pt(DACH)(Ox)(OEt)(SucTPP)] in high purity. Conjugation of TPP to c,c,t-[Pt(DACH)(Ox)(OEt)(Suc)] was demonstrated to ameliorate its inherent cytotoxicity fifteen fold in the Pt sensitive HCT116 colorectal cancer cell line and two fold in the relatively resistant HT29 colorectal cancer cell line.

Funding

RCSI Apjohn Scholarship

Science Foundation Ireland (Grant Number 12/IP/1305 & Grant Number 16/RI/3737)

Synthesis and Solid State Pharmaceutical Centre (SSPC), financed by a research grant from Science Foundation Ireland (SFI) and co-funded under the European Regional Development Fund under Grant Number 12/RC/2275_P2

History

Comments

The original article is available at https://www.sciencedirect.com/

Published Citation

Kitteringham E, McKeon AM, O’Dowd P, Devocelle M, Murphy BM, Griffith DM. Synthesis and characterisation of a novel mono functionalisable Pt(IV) oxaliplatin-type complex and its peptide conjugate. Inorganica Chimica Acta. 2020;505:119492

Publication Date

1 February 2020

Department/Unit

  • Chemistry
  • Physiology and Medical Physics

Research Area

  • Cancer
  • Chemistry and Pharmaceutical Sciences

Publisher

Elsevier BV

Version

  • Accepted Version (Postprint)