Download MendeleyAntagonists of inhibitor of apoptosis proteins based on thiazole amide isosteres.
Cohen, F., Koehler, M.F., Bergeron, P., Elliott, L.O., Flygare, J.A., Franklin, M.C., Gazzard, L., Keteltas, S.F., Lau, K., Ly, C.Q., Tsui, V., Fairbrother, W.J.(2010) Bioorg Med Chem Lett 20: 2229-2233
- PubMed: 20189383
- DOI: https://doi.org/10.1016/j.bmcl.2010.02.021
- Primary Citation of Related Structures:
3GT9, 3GTA - PubMed Abstract:
A series of IAP antagonists based on thiazole or benzothiazole amide isosteres was designed and synthesized. These compounds were tested for binding to the XIAP-BIR3 and ML-IAP BIR using a fluorescence polarization assay. The most potent of these compounds, 19a and 33b, were found to have K(i)'s of 20-30 nM against ML-IAP and 50-60 nM against XIAP-BIR3.
Organizational Affiliation:
Department of Discovery Chemistry, Genentech, Inc. 1 DNA Way, South San Francisco, CA 94080, USA. fcohen@gene.com
