RESUMEN
A thiophene-phenylquinoline-based homoleptic Ir(III) complex, [Ir(Th-PQ)(3)], has been synthesised by a simple route and utilised as a dopant in solution-processed phosphorescent organic light-emitting diodes (PhOLEDs). It shows the current efficiency of approximately 26â cd A(-1) and the external quantum efficiency of about 21 %, which are the highest values reported to date for PhOLEDs prepared by solution-process.
RESUMEN
Because androgen receptor (AR) signalling is important for the development and progression of prostate cancer (PC), AR antagonists are utilized in clinical practices to treat PC and are referred to as androgen deprivation therapy (ADT). However, continued administration of AR antagonists often results in the development of resistance, known as castration-resistant prostate cancer (CRPC). Despite castration, it has been demonstrated that AR signalling continues to be fundamental to tumour growth. In this regard, a series of readily synthesizable 4,4-dimethylimidazolidine-2-one pharmacophore-based AR antagonists (FAR01-FAR11) were designed and synthesized. Androgen-dependent LNCaP PC cell line was used to test the AR-antagonist activity of these compounds in vitro and compared with the U.S. Food and Drug Administration (FDA) approved second-generation enzalutamide. In our previous work, rigid thiohydantoin pharmacophore in enzalutamide is replaced by the flexible 4,4-dimethylimidazolidin-2-one. In order to improve the flexibility further, one methylene group is introduced between the pharmacophore and one of the aromatic ring. Despite the fact that the amide functional group is a crucial characteristic for building AR antagonists, this class of molecules lacks one. FAR06 has the exact same activity as enzalutamide (IC50 : 0.782 µM) with an IC50 value of 0.801 µM among the series of compounds.
Asunto(s)
Antagonistas de Receptores Androgénicos , Neoplasias de la Próstata Resistentes a la Castración , Masculino , Humanos , Antagonistas de Receptores Androgénicos/farmacología , Antagonistas de Receptores Androgénicos/uso terapéutico , Neoplasias de la Próstata Resistentes a la Castración/tratamiento farmacológico , Receptores Androgénicos/metabolismo , Andrógenos/metabolismo , Andrógenos/farmacología , Andrógenos/uso terapéutico , Antagonistas de Andrógenos/farmacología , Farmacóforo , Nitrilos , Línea Celular Tumoral , Resistencia a AntineoplásicosRESUMEN
An oxadiazole based electron transporting (ET) unit was glued to the heteroleptic Ir(III) complex (TPQIr-ET) and used as a dopant for phosphorescent organic light-emitting diodes (PhOLEDs). It shows superior device performance than the dopant without the ET unit (TPQIr) due to the balanced charge carrier injection by the ET unit.