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1.
Molecules ; 23(9)2018 Aug 29.
Artículo en Inglés | MEDLINE | ID: mdl-30158487

RESUMEN

Efficient metal catalyzed C⁻H arylation of 8-alkyl-thiazolo[5,4-f]-quinazolin-9-ones was explored for SAR studies. Application of this powerful chemical tool at the last stage of the synthesis of kinase inhibitors allowed the synthesis of arrays of molecules inspired by fragment-growing studies generated by molecular modeling calculations. Among the potentially active compounds designed through this strategy, FC162 (4c) exhibits nanomolar IC50 values against some kinases, and is the best candidate for the development as a DYRK kinase inhibitor.


Asunto(s)
Inhibidores de Proteínas Quinasas/síntesis química , Quinazolinas/síntesis química , Microondas , Modelos Moleculares , Simulación del Acoplamiento Molecular , Estructura Molecular , Inhibidores de Proteínas Quinasas/química , Proteínas Serina-Treonina Quinasas/antagonistas & inhibidores , Proteínas Tirosina Quinasas/antagonistas & inhibidores , Quinazolinas/química , Relación Estructura-Actividad , Quinasas DyrK
2.
Org Lett ; 18(13): 3282-5, 2016 07 01.
Artículo en Inglés | MEDLINE | ID: mdl-27314437

RESUMEN

A selective functionalization of thiazolo[5,4-f]quinazolin-9(8H)-one has been developed through sequential activation of C-H bonds to furnish diarylated compounds. This strategy allows the regioselective C2 and C7 arylation by a judicious choice of coupling partners and bases, requiring no additional ligands or directing groups. Differently substituted N(8)-benzylated-2,7-diaryl-thiazoloquinazolin-9(8H)-ones were thereby obtained in a facile manner. A one-pot procedure was also performed. These protocols provide a synthetically useful route for late-stage functionalization of this highly valuable scaffold, required in drug discovery.

3.
Org Lett ; 17(7): 1700-3, 2015 Apr 03.
Artículo en Inglés | MEDLINE | ID: mdl-25781369

RESUMEN

A microwave-assisted method for the palladium-catalyzed direct arylation of quinazolin-4-one has been developed under copper-assistance. This method is applicable to a wide range of aryl iodides and substituted (2H)-quinazolin-4-ones. This protocol provides a simple and efficient way to synthesize biologically relevant 2-arylquinazolin-4-one backbones.


Asunto(s)
Cobre/química , Yoduros/química , Paladio/química , Quinazolinonas/química , Catálisis , Enlace de Hidrógeno , Microondas , Estructura Molecular
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