Strategies for improving the solubility and metabolic stability of griseofulvin analogues.
Eur J Med Chem
; 116: 210-215, 2016 Jun 30.
Article
em En
| MEDLINE
| ID: mdl-27061984
ABSTRACT
We report two types of modifications to the natural product griseofulvin as strategies to improve solubility and metabolic stability the conversion of aryl methyl ethers into aryl difluoromethyl ethers at metabolic hotspots and the conversion of the C-ring ketone into polar oximes. The syntheses of the analogues are described together with their solubility, metabolic half-life in vitro and antiproliferative effect in two cancer cell lines. We conclude that on balance, the formation of polar oximes is the most promising strategy for improving the properties of the analogues.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Griseofulvina
/
Antineoplásicos
Limite:
Animals
/
Humans
/
Male
Idioma:
En
Revista:
Eur J Med Chem
Ano de publicação:
2016
Tipo de documento:
Article
País de afiliação:
Dinamarca