Novel Planar Pt(II) Cyclometallated Cytotoxic Complexes with G-Quadruplex Stabilisation and Luminescent Properties.

ABSTRACT: Herein is described the development of a series of novel quadruplex DNA (QDNA)-stabilising cyclometallated square-planar metal complexes (CMCs). Melting experiments using quadruplex DNA (QDNA) demonstrated that interactions with the complexes increased the melting temperature by up to 19 °C. This QDNA stabilisation was determined in two of the major G-quadruplex structures formed in the human c-MYC promoter gene (c-MYC) and a human telomeric repeat sequence (H-Telo). The CMCs were found to stabilise H-telo more strongly than c-MYC, and the CMCs with the highest cytotoxic effect had a low-moderate correlation between H-telo binding capacity and cytotoxicity (R² values up to 10 times those of c-MYC). The melting experiments further revealed that the stabilisation effect was altere

SUBMITTER: McGhie BS 

PROVIDER: S-EPMC9499473 | biostudies-literature | 2022 Sep

REPOSITORIES: biostudies-literature