In this section
@article{Vilar:2024:10.1002/chem.202402465,
author = {Vilar, R and Bartlett, M and Burke, J and Sherin, P and Kuimova, MK and Barahona, M},
doi = {10.1002/chem.202402465},
journal = {Chemistry: A European Journal},
title = {Platinum(II)-Salphen complexes as DNA binders and photosensitisers},
url = {http://dx.doi.org/10.1002/chem.202402465},
year = {2024}
}
TY - JOUR
AB - Current anticancer therapies suffer from issues such as off-target side effects and the emergence of drug resistance; therefore, the discovery of alternative therapeutic approaches is vital. These can include the development of drugs with different modes of action, and the exploration of new biomolecular targets. For the former, there has been increasing interest in drugs that are activated by an external stimulus to generate cytotoxic species. For the latter, significant efforts are being directed to explore non-canonical DNA and RNA structures (e.g. guanine-quadruplexes), as alternative biomolecular targets. Herein we report the synthesis of a library of 21 new platinum(II)-Salphen complexes, investigation of their photophysical and photochemical properties, their interactions with duplex and quadruplex DNA, and their cytotoxicity against HeLa cancer cells in the dark and upon light irradiation. Thanks to the intrinsic phosphorescence of the platinum(II) complexes, confocal microscopy was used for six of the complexes to determine their cellular permeability and localisation in two cancer cell lines. These studies have allowed us to identify two lead platinum(II) complexes with high guanine-quadruplex DNA affinity and selectivity, good cell permeability and nuclear localisation, and high cytotoxicity against HeLa cancer cells upon irradiation with no detected cytotoxicity in the dark.
AU - Vilar,R
AU - Bartlett,M
AU - Burke,J
AU - Sherin,P
AU - Kuimova,MK
AU - Barahona,M
DO - 10.1002/chem.202402465
PY - 2024///
SN - 0947-6539
TI - Platinum(II)-Salphen complexes as DNA binders and photosensitisers
T2 - Chemistry: A European Journal
UR - http://dx.doi.org/10.1002/chem.202402465
UR - https://www.ncbi.nlm.nih.gov/pubmed/39115950
UR - https://chemistry-europe.onlinelibrary.wiley.com/doi/10.1002/chem.202402465
UR - http://hdl.handle.net/10044/1/113841
ER -