Optimizing thiadiazole analogues of resveratrol versus three chemopreventive targets.
Bioorg Med Chem
; 20(1): 510-20, 2012 Jan 01.
Article
em En
| MEDLINE
| ID: mdl-22115839
ABSTRACT
Chemoprevention is an approach to decrease cancer morbidity and mortality through inhibition of carcinogenesis and prevention of disease progression. Although the trans stilbene derivative resveratrol has chemopreventive properties, its action is compromised by weak non-specific effects on many biological targets. Replacement of the stilbene ethylenic bridge of resveratrol with a 1,2,4-thiadiazole heterocycle and modification of the substituents on the two aromatic rings afforded potential chemopreventive agents with enhanced potencies and selectivities when evaluated as inhibitors of aromatase and NF-κB and inducers of quinone reductase 1 (QR1).
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Estilbenos
/
Tiadiazóis
/
Neoplasias
/
Antineoplásicos
Tipo de estudo:
Prognostic_studies
Limite:
Humans
Idioma:
En
Ano de publicação:
2012
Tipo de documento:
Article