Discovery of 9,10-Dihydroacridines as Novel Class of ABCB1 Inhibitors.
Med Chem
; 11(4): 329-35, 2015.
Article
en En
| MEDLINE
| ID: mdl-25391533
ABSTRACT
Nonplanar 9,10-dihydroacridines were synthesized as promising C2 symmetric molecular scaffolds as inhibitors of the transmembrane efflux pump ABCB1. Within the series structure-activity relationships are discussed revealing the importance of hydrogen bond acceptor functions. A selectivity of ABCB1 inhibition is demonstrated for selected candidates and a bioanalytical study proved nontoxicity as well as missing ABCB1 substrate properties. The results encourage to further develop the promising class of ABCB1 inhibitors.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Acridinas
/
Proteínas de Neoplasias
/
Antineoplásicos
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Med Chem
Asunto de la revista:
QUIMICA
Año:
2015
Tipo del documento:
Article