Non-peptidic small molecule inhibitors of XIAP

Non-peptidic small molecule SMAC mimetics were designed and synthesized that bind to the BIR3 domain of XIAP using structure-based design. Substituted five-membered heterocycles such as thiazoles and imidazoles were identified that serve as replacements for peptide fragments of the lead. Non-peptidi...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2005-02, Vol.15 (3), p.771-775
Hauptverfasser:	Park, Cheol-Min, Sun, Chaohong, Olejniczak, Edward T., Wilson, Alan E., Meadows, Robert P., Betz, Stephen F., Elmore, Steven W., Fesik, Stephen W.
Format:	Artikel
Sprache:	eng
Schlagworte:	Antineoplastic agents Binding Sites Biological and medical sciences Drug Design General aspects Heterocyclic Compounds - chemical synthesis Heterocyclic Compounds - pharmacology Humans Imidazoles - chemical synthesis Imidazoles - pharmacology Ligands Magnetic Resonance Spectroscopy Medical sciences Pharmacology. Drug treatments Proteins - antagonists & inhibitors SMAC mimetics Structure-Activity Relationship Thiazoles - chemical synthesis Thiazoles - pharmacology X-Linked Inhibitor of Apoptosis Protein XIAP inhibitors
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Beschreibung
Zusammenfassung:	Non-peptidic small molecule SMAC mimetics were designed and synthesized that bind to the BIR3 domain of XIAP using structure-based design. Substituted five-membered heterocycles such as thiazoles and imidazoles were identified that serve as replacements for peptide fragments of the lead. Non-peptidic small molecule SMAC mimetics were designed and synthesized that bind to the BIR3 domain of XIAP using structure-based design. Substituted five-membered heterocycles such as thiazoles and imidazoles were identified that serve as replacements for peptide fragments of the lead.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2004.11.010