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Thiourea and Guanidine Compounds and their Iridium Complexes in Drug-Resistant Cancer Cell Lines: Structure-Activity Relationships and Direct Luminescent Imaging

preprint
submitted on 10.07.2019 and posted on 11.07.2019 by Samuel J. Thomas, Barbora Balonova, Jindrich Cinatl, Mark Wass, Christopher Serpell, Barry Blight, Martin Michaelis

Thiourea and guanidine units are found in nature, medicine, and materials. Their continued exploration in applications as diverse as cancer therapy, sensors, and electronics means that their toxicity is an important consideration. We have systematically synthesised a set of thiourea compounds and their guanidine analogues, and elucidated structure-activity relationships in terms of cellular toxicity in three ovarian cancer cell lines and their cisplatin-resistant sub-lines. We have been able to use the intrinsic luminescence of iridium complexes to visualise the effect of both structure alteration and cellular resistance mechanisms. These findings provide starting points for the development of new drugs and consideration of safety issues for novel thiourea- and guanidine-based materials.

Funding

SACO AEI Polymers UK, Frankfurter Stiftung für krebskranke Kinder, and Hilfe für krebskranke Kinder Frankfurt e.V

History

Email Address of Submitting Author

c.j.serpell@kent.ac.uk

Institution

University of Kent

Country

UK

ORCID For Submitting Author

0000-0002-2848-9077

Declaration of Conflict of Interest

No conflicts of interest.

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