Non-peptidic small molecule inhibitors of XIAP

Cheol-Min Park; Chaohong Sun; Edward T Olejniczak; Alan E Wilson; Robert P Meadows; Stephen F Betz; Steven W Elmore; Stephen W Fesik

doi:10.1016/j.bmcl.2004.11.010

Non-peptidic small molecule inhibitors of XIAP

Bioorg Med Chem Lett. 2005 Feb 1;15(3):771-5. doi: 10.1016/j.bmcl.2004.11.010.

Authors

Cheol-Min Park¹, Chaohong Sun, Edward T Olejniczak, Alan E Wilson, Robert P Meadows, Stephen F Betz, Steven W Elmore, Stephen W Fesik

Affiliation

¹ Cancer Research, Global Pharmaceutical R and D, Abbott Laboratories, 100 Abbott Park Rd, Abbott Park, IL 60064-6010, USA. cheol-min.park@abbott.com

PMID: 15664855
DOI: 10.1016/j.bmcl.2004.11.010

Abstract

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.

MeSH terms

Binding Sites
Drug Design
Heterocyclic Compounds / chemical synthesis*
Heterocyclic Compounds / pharmacology
Humans
Imidazoles / chemical synthesis
Imidazoles / pharmacology
Ligands
Magnetic Resonance Spectroscopy
Proteins / antagonists & inhibitors*
Structure-Activity Relationship
Thiazoles / chemical synthesis
Thiazoles / pharmacology
X-Linked Inhibitor of Apoptosis Protein

Substances

Heterocyclic Compounds
Imidazoles
Ligands
Proteins
Thiazoles
X-Linked Inhibitor of Apoptosis Protein
XIAP protein, human