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
em 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.
Texto completo:
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Base de dados:
MEDLINE
Assunto principal:
Prolina
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Proteínas Inibidoras de Apoptose
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Descoberta de Drogas
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Neoplasias Experimentais
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Antineoplásicos
Idioma:
En
Ano de publicação:
2015
Tipo de documento:
Article