Discovery of potent heterodimeric antagonists of inhibitor of apoptosis proteins (IAPs) with sustained antitumor activity.
J Med Chem
; 58(3): 1556-62, 2015 Feb 12.
Article
de En
| MEDLINE
| ID: mdl-25584393
ABSTRACT
The prominent role of IAPs in controlling cell death and their overexpression in a variety of cancers has prompted the development of IAP antagonists as potential antitumor therapies. We describe the identification of a series of heterodimeric antagonists with highly potent antiproliferative activities in cIAP- and XIAP-dependent cell lines. Compounds 15 and 17 further demonstrate curative efficacy in human melanoma and lung cancer xenograft models and are promising candidates for advanced studies.
Texte intégral:
1
Collection:
01-internacional
Base de données:
MEDLINE
Sujet principal:
Proline
/
Protéines IAP
/
Découverte de médicament
/
Tumeurs expérimentales
/
Antinéoplasiques
Limites:
Animals
/
Humans
Langue:
En
Journal:
J Med Chem
Sujet du journal:
QUIMICA
Année:
2015
Type de document:
Article
Pays d'affiliation:
États-Unis d'Amérique