Design and campaign synthesis of pyridine-based histone deacetylase inhibitors.
Bioorg Med Chem Lett
; 18(8): 2525-9, 2008 Apr 15.
Article
de En
| MEDLINE
| ID: mdl-18378451
ABSTRACT
A lead benzamide, bearing a cyanopyridyl moiety (3), was identified as a potent and low molecular weight histone deacetylase (HDAC) inhibitor. Various replacements of the cyano group were explored at the C3-position, along with the exploration of solubility-enhancing groups at the C5-position. It was determined that cyano substitution at the C3-position of the pyridyl core, along with a methylazetidinyl substituent at the C5-position yielded optimal HDAC1 inhibition and anti-proliferative activity in HCT-116 cells.
Texte intégral:
1
Collection:
01-internacional
Base de données:
MEDLINE
Sujet principal:
Pyridines
/
Conception de médicament
/
Antienzymes
/
Inhibiteurs de désacétylase d'histone
Limites:
Animals
/
Humans
Langue:
En
Journal:
Bioorg Med Chem Lett
Sujet du journal:
BIOQUIMICA
/
QUIMICA
Année:
2008
Type de document:
Article
Pays d'affiliation:
Royaume-Uni