Elaboration of tetra-orthogonally-substituted aromatic scaffolds towards novel EGFR-kinase inhibitors.
Org Biomol Chem
; 14(35): 8246-52, 2016 Sep 21.
Article
em En
| MEDLINE
| ID: mdl-27453149
ABSTRACT
Nitration of three regioisomers of bromo-fluorobenzaldehyde proceeds regioselectively, notably with H2SO4/HNO3 at 0 °C. The thereby synthesized tetrasubstituted aromatics, endowed with orthogonal substituents, can be elaborated via Pd-catalysed coupling, reduction and reductive amination reactions. As a test-case, these compounds were converted into EGFR inhibitors related to Gefitinib, whose activity was rationalised by docking studies.
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Base de dados:
MEDLINE
Assunto principal:
Inibidores de Proteínas Quinases
/
Bibliotecas de Moléculas Pequenas
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Receptores ErbB
Limite:
Animals
/
Humans
Idioma:
En
Ano de publicação:
2016
Tipo de documento:
Article