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Full-Text Articles in Medicinal-Pharmaceutical Chemistry

Directed Self-Assembly Of Fluorescence Responsive Nanoparticles And Their Use For Real-Time Surface And Cellular Imaging., Shane Cheung, Donal F. O'Shea Dec 2017

Directed Self-Assembly Of Fluorescence Responsive Nanoparticles And Their Use For Real-Time Surface And Cellular Imaging., Shane Cheung, Donal F. O'Shea

Chemistry Articles

Directed self-assemblies in water are known as the most efficient means of forming complex higher ordered structures in nature. Here we show a straightforward and robust method for particle assembly which utilises the amphiphilic tri-block co-polymer poloxamer-188 and a hydrophobic fluorophore as the two designer components, which have a built-in ability to convey spatial and temporal information about their surroundings to an observer. Templating of particle self-assembly is attributed to interactions between the fluorophore and hydrophobic segment of the poloxamer. Particle fluorescence in water is quenched but can be induced to selectively switch on in response to temperature, surface adsorption ...


Platinum(Iv) Oxaliplatin-Peptide Conjugates Targeting Memhsp70+ Phenotype In Colorectal Cancer Cells., Aoife M. Mckeon, Janis Noonan, Marc Devocelle, Brona M. Murphy, Darren M. Griffith Oct 2017

Platinum(Iv) Oxaliplatin-Peptide Conjugates Targeting Memhsp70+ Phenotype In Colorectal Cancer Cells., Aoife M. Mckeon, Janis Noonan, Marc Devocelle, Brona M. Murphy, Darren M. Griffith

Chemistry Articles

Novel Pt(iv) tumour penetrating peptide (TPP) conjugates are reported. They are the first example of metallodrugs to target a membrane bound heat shock protein 70 positive (memHSP70+) phenotype in cancer cells. The conjugates exhibit superior cytotoxicity as compared to oxaliplatin alone in Pt resistant colorectal cancer cells with relatively high memHSP70+ expression. Substitution of TPP in Pt(iv) peptide conjugates with scrambled peptide (ScP) essentially abolishes the observed cytotoxicity.


Bf2-Azadipyrromethene Nir-Emissive Fluorophores With Research And Clinical Potential., Harrison C. Daly, Gonzalo Sampedro, Corentin Bon, Dan Wu, Ghazi Ismail, Ronan A. Cahill, Donal F. O'Shea Jul 2017

Bf2-Azadipyrromethene Nir-Emissive Fluorophores With Research And Clinical Potential., Harrison C. Daly, Gonzalo Sampedro, Corentin Bon, Dan Wu, Ghazi Ismail, Ronan A. Cahill, Donal F. O'Shea

Chemistry Articles

The use of near-infrared fluorescence for in vivo research and intraoperative clinical imaging is rapidly expanding, with new applications being proposed and developed. While imaging hardware and software have significantly progressed in recent times, the molecular fluorescent agents remain a limiting factor. In this report, the design, synthesis, photophysical characterization and bio-medical imaging assessment of two new NIR-fluorophores based on the BF


Mandelic Acid Derived Ionic Liquids: Synthesis, Toxicity And Biodegradability, Hannah Prydderch, Annette Haib, Marcel Spulak, Brid Quilty, Klaus Kummerer, Andreas Heise, Nicholas Gathergood Jan 2017

Mandelic Acid Derived Ionic Liquids: Synthesis, Toxicity And Biodegradability, Hannah Prydderch, Annette Haib, Marcel Spulak, Brid Quilty, Klaus Kummerer, Andreas Heise, Nicholas Gathergood

Chemistry Articles

A series of ten ionic liquids (ILs) was synthesised from the renewable resource mandelic acid. The ILs showed low antimicrobial activity towards the thirteen bacterial and twelve fungal strains they were screened against. A general trend of increasing bacterial toxicity in the order methyl ester < ethyl ester < n-butyl ester/amide was observed. IL biodegradability was evaluated using the Closed Bottle test (OECD 301D). Biodegradation increased in the order of increasing alkyl chain length for the ester ILs (methyl < ethyl < n-butyl). Despite none of the ILs presenting as readily biodegradable (>60% in 28 days), a series of biodegradation transformation products has been proposed based on the degradation of the ester/ amide alkyl chain. This data has allowed for an assessment of the effect of IL structural features on toxicity and biodegradation, particularly allowing for a comparison to earlier work where additional oxygen atoms were present ...


Fluorogenic Nir-Probes Based On 1,2,4,5-Tetrazine Substituted Bf2-Azadipyrromethenes, Dan Wu, Donal F. O'Shea Jan 2017

Fluorogenic Nir-Probes Based On 1,2,4,5-Tetrazine Substituted Bf2-Azadipyrromethenes, Dan Wu, Donal F. O'Shea

Chemistry Articles

A series of 1,2,4,5-tetrazine integrated near infrared (NIR) fluorophores based on the BF2 azadipyrromethene (NIR-AZA) class has been synthesised and their ability to modulate emission from low to high in response to Diels-Alder cycloaditions has been assessed. Substituents on the tetrazine component of the probe (Cl, OMe, p-NO2C6H4O) were seen to strongly influence quantum yields, fluorescence enhancement factors, and rates of cycloadditions. Cycloadditions between tetrazine-NIR-AZA constructs and a strained alkyne substrate were seen to be highly efficient in organic or aqueous solutions and in gels with high fluorescence enhancements of up to 48-fold observed. Real-time demonstration of ...


Polymer Brush Decorated Nanoparticles Immobilised On Polymer Monoliths For Enhanced Biopolymer Elution, M Iacono, D Connolly, Andreas Heise Jan 2017

Polymer Brush Decorated Nanoparticles Immobilised On Polymer Monoliths For Enhanced Biopolymer Elution, M Iacono, D Connolly, Andreas Heise

Chemistry Articles

A protocol for the decoration of a polymeric monolith with polymer brush grafted silica nanoparticles was developed. Monolithic poly(glycidyl methacrylate-co-ethylene glycol dimethacrylate) (GMA-co-EDMA) was prepared in 15 mm long cylindrical polypropylene tubing and quarternized. 160 nm silica nanoparticles with a 20 nm poly(methacrylic acid-co-tert-butyl methacrylate) brush layer were flushed through the monolith and electrostatically trapped. A uniform and dense carboxylic acid containing brush nanoparticle surface decoration over the entire length of the monolith was achieved. Elution performance of the brush nanoparticle decorated monolith was compared to a carboxylic acid surface decorated monolith ...