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Bioorg Med Chem Lett. 2008 Dec 15;18(24):6352-6. doi: 10.1016/j.bmcl.2008.10.092. Epub 2008 Nov 1.

Identification and optimization of N3,N6-diaryl-1H-pyrazolo[3,4-d]pyrimidine-3,6-diamines as a novel class of ACK1 inhibitors.

Author information

1
Department of Chemistry, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA. dkopecky@amgen.com

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.

PMID:
18993068
DOI:
10.1016/j.bmcl.2008.10.092
[Indexed for MEDLINE]

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