Ring size changes in the development of class I HDAC inhibitors.
J Enzyme Inhib Med Chem
; 36(1): 1387-1401, 2021 Dec.
Article
em En
| MEDLINE
| ID: mdl-34167419
ABSTRACT
Five pathways involving different ring structures led to generation of fourteen thienylbenzamides (7-20) which display the structure-activity relationships of class I HDAC inhibitors. All the synthesised compounds inhibit HDAC1 and HDAC2 selectively over other isoforms and many inhibit DLD1 and HCT116 cells more effectively than a parent compound. Compounds 8 and 16 inhibit HCT116 cells by activation of the apoptosis pathway.
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Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Inibidores de Histona Desacetilases
/
Desenvolvimento de Medicamentos
Limite:
Humans
Idioma:
En
Ano de publicação:
2021
Tipo de documento:
Article