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Design, Synthesis and Evaluation of Tricyclic, Conformationally Constrained Small-Molecule Mimetics of Second Mitochondria-derived Activator of Caspases
A series of tricyclic, conformationally constrained Smac mimetics have been designed, synthesized and evaluated. The most potent compound 6 (WS-5) binds to XIAP, cIAP-1 and cIAP-2 with K(i) values of 18, 1.1 and 4.2 nM, respectively. Compound 6 antagonizes XIAP in a functional assay and induces cIAP...
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| Main Authors: | , , , , , , , , |
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| Formato: | Artigo |
| Idioma: | Inglês |
| Publicado em: |
2008
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| Assuntos: | |
| Acesso em linha: | https://ncbi.nlm.nih.gov/pmc/articles/PMC2662380/ https://ncbi.nlm.nih.gov/pubmed/19012392 https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm801146d |
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