Monofunctional platinum(ii) anticancer complexes based on multidentate phenanthridine-containing ligand frameworks

Issiah B Lozada; Bin Huang; Morgan Stilgenbauer; Travis Beach; Zihan Qiu; Yaorong Zheng; David E Herbert

doi:10.1039/d0dt01275k

Monofunctional platinum(ii) anticancer complexes based on multidentate phenanthridine-containing ligand frameworks

Dalton Trans. 2020 May 26;49(20):6557-6560. doi: 10.1039/d0dt01275k.

Authors

Issiah B Lozada¹, Bin Huang¹, Morgan Stilgenbauer², Travis Beach², Zihan Qiu², Yaorong Zheng², David E Herbert¹

Affiliations

¹ Department of Chemistry and the Manitoba Institute for Materials, University of Manitoba, 144 Dysart Road, Winnipeg, Manitoba R3T 2N2, Canada.
² Department of Chemistry, Kent State University, Kent, Ohio 44240, USA. david.herbert@umanitoba.ca.

PMID: 32342084
DOI: 10.1039/d0dt01275k

Abstract

Phenanthriplatin is a leading preclinical anticancer Pt complex distinguished by a phenanthridine ligand that facilitates DNA-targeted covalent binding via intercalation. We report here that Pt(ii) complexes incorporating phenanthridine into a chelating, multidentate ligand scaffold exhibit a superior in vitro therapeutic index compared with phenanthriplatin and cisplatin.

MeSH terms

Antineoplastic Agents / chemical synthesis
Antineoplastic Agents / chemistry
Antineoplastic Agents / pharmacology*
Apoptosis / drug effects
Cell Line, Tumor
Cell Proliferation / drug effects
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
HEK293 Cells
Humans
Ligands
Molecular Structure
Organoplatinum Compounds / chemical synthesis
Organoplatinum Compounds / chemistry
Organoplatinum Compounds / pharmacology*
Phenanthridines / chemistry
Phenanthridines / pharmacology*
Structure-Activity Relationship

Substances

Antineoplastic Agents
Ligands
Organoplatinum Compounds
Phenanthridines