Thiourea and Guanidine Compounds and their Iridium Complexes in Drug-Resistant Cancer Cell Lines: Structure-Activity Relationships and Direct Luminescent Imaging
Autor: | Christopher J. Serpell, Samuel J. Thomas, Mark N. Wass, Jindrich Cinatl, Martin Michaelis, Barry A. Blight, Barbora Balónová |
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Rok vydání: | 2019 |
Předmět: |
Intrinsic luminescence
Cancer therapy chemistry.chemical_element Antineoplastic Agents Drug resistance Iridium 01 natural sciences Biochemistry Structure-Activity Relationship chemistry.chemical_compound Coordination Complexes Cell Line Tumor Neoplasms Drug Discovery Humans QD General Pharmacology Toxicology and Pharmaceutics Guanidine Cell Proliferation Pharmacology Microscopy Confocal Dose-Response Relationship Drug Molecular Structure 010405 organic chemistry Optical Imaging Organic Chemistry Thiourea Combinatorial chemistry 0104 chemical sciences 010404 medicinal & biomolecular chemistry Drug development chemistry Drug Resistance Neoplasm Molecular Medicine Drug Screening Assays Antitumor Cancer cell lines Luminescence |
ISSN: | 1860-7179 |
Popis: | 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. Iridium complexes present new opportunities for drug development and imaging in terms of structure and photoactivity. We have systematically synthesised a set of thiourea and guanidine compounds and iridium complexes thereof, and elucidated structure-activity relationships for 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-, guanidine-, and iridium-based materials. |
Databáze: | OpenAIRE |
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