Synthesis and characterisation of a novel mono functionalisable Pt(IV) oxaliplatin-type complex and its peptide conjugate
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 GriffithThe 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;505:119492Publication Date
1 February 2020External DOI
Department/Unit
- Chemistry
- Physiology and Medical Physics
Research Area
- Cancer
- Chemistry and Pharmaceutical Sciences
Publisher
Elsevier BVVersion
- Accepted Version (Postprint)
