Download MendeleyIdentification and optimization of N3,N6-diaryl-1H-pyrazolo[3,4-d]pyrimidine-3,6-diamines as a novel class of ACK1 inhibitors.
Kopecky, D.J., Hao, X., Chen, Y., Fu, J., Jiao, X., Jaen, J.C., Cardozo, M.G., Liu, J., Wang, Z., Walker, N.P., Wesche, H., Li, S., Farrelly, E., Xiao, S.H., Kayser, F.(2008) Bioorg Med Chem Lett 18: 6352-6356
- PubMed: 18993068
- DOI: https://doi.org/10.1016/j.bmcl.2008.10.092
- Primary Citation of Related Structures:
3EQP, 3EQR - PubMed Abstract:
A new series of pyrazolo[3,4-d]pyrimidine-3,6-diamines was designed and synthesized as potent and selective inhibitors of the nonreceptor tyrosine kinase, ACK1. These compounds arose from efforts to rigidify an earlier series of N-aryl pyrimidine-5-carboxamides. The synthesis and structure-activity relationships of this new series of inhibitors are reported. The most promising compounds were also profiled for their pharmacokinetic properties.
Organizational Affiliation:
Department of Chemistry, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA. dkopecky@amgen.com
