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1.
Molecules ; 25(18)2020 Sep 16.
Artículo en Inglés | MEDLINE | ID: mdl-32947960

RESUMEN

The relaxivity of MRI contrast agents can be increased by increasing the size of the contrast agent and by increasing concentration of the bound gadolinium. Large multi-site ligands able to coordinate several metal centres show increased relaxivity as a result. In this paper, an "aza-type Michael" reaction is used to prepare cyclen derivatives that can be attached to organosilicon frameworks via hydrosilylation reactions. A range of organosilicon frameworks were tested including silsesquioxane cages and dimethylsilylbenzene derivatives. Michael donors with strong electron withdrawing groups could be used to alkylate cyclen on three amine centres in a single step. Hydrosilylation successfully attached these to mono-, di-, and tri-dimethylsilyl-substituted benzene derivatives. The europium and gadolinium complexes were formed and studied using luminescence spectroscopy and relaxometry. This showed the complexes to contain two bound water moles per lanthanide centre and T1 relaxation time measurements demonstrated an increase in relaxivity had been achieved, in particular for the trisubstituted scaffold 1,3,5-tris((pentane-sDO3A)dimethylsilyl)benzene-Gd3. This showed a marked increase in the relaxivity (13.1 r1p/mM-1s-1).


Asunto(s)
Medios de Contraste/química , Europio/química , Gadolinio/química , Compuestos de Organosilicio/química , Derivados del Benceno/química , Medios de Contraste/síntesis química , Complejos de Coordinación/síntesis química , Complejos de Coordinación/química , Ligandos
2.
Sci Prog ; 99(4): 351-398, 2016 12 01.
Artículo en Inglés | MEDLINE | ID: mdl-28742478

RESUMEN

There are over 2.6 million users of e-cigarettes in the United Kingdom alone as they have been promoted as a safer alternative to traditional cigarettes. The addition of flavours and aromas has also proven to be popular with younger generations. In this review, we survey the range of studies in the short timeframe since e-cigarettes reached the market to draw attention to the health associated risks and benefits of their introduction. We complement this review with a case study reporting on the composition of selected e-cigarette refills with particular emphasis on the toxicological activity of its components on lung cells.


Asunto(s)
Bronquios/efectos de los fármacos , Sistemas Electrónicos de Liberación de Nicotina , Epitelio/efectos de los fármacos , Aromatizantes/toxicidad , Fumar/efectos adversos , Animales , Línea Celular , Modelos Animales de Enfermedad , Relación Dosis-Respuesta a Droga , Aromatizantes/análisis , Glicerol/análisis , Glicerol/toxicidad , Humanos , Concentración 50 Inhibidora , Hígado/efectos de los fármacos , Pulmón/efectos de los fármacos , Metales/análisis , Metales/toxicidad , Ratones , Nicotina/análisis , Nicotina/toxicidad , Propilenglicol/análisis , Propilenglicol/toxicidad , Reino Unido
3.
Anticancer Res ; 36(11): 6043-6050, 2016 11.
Artículo en Inglés | MEDLINE | ID: mdl-27793931

RESUMEN

Childhood bone cancer though rare, has very limited treatment choices, with poor survival rates and often involving amputation. We developed a novel molecule, 2', 4'-dihydroxy-dithion-dibenzoyl-methane and tested it on hepatic, colon, lung and osteoblast cancer cell lines. Thionylation of 2', 4'- dihydroxydibenzoylmethane led to selective targeting of bone cancer cells, stopping their growth and leading to their death without affecting non-cancerous cells within the bone marrow or other non-malignant cells.


Asunto(s)
Antineoplásicos/uso terapéutico , Neoplasias Óseas/tratamiento farmacológico , Chalconas/uso terapéutico , Línea Celular Tumoral , Niño , Humanos
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