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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.
Artigo em Inglês | 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.
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Texto completo: Disponível Coleções: Bases de dados internacionais Base de dados: MEDLINE Assunto principal: Prolina / Proteínas Inibidoras de Apoptose / Descoberta de Drogas / Neoplasias Experimentais / Antineoplásicos Limite: Animais / Humanos Idioma: Inglês Revista: J Med Chem Assunto da revista: Química Ano de publicação: 2015 Tipo de documento: Artigo País de afiliação: Estados Unidos