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Bioorg Med Chem Lett. 2012 Oct 1;22(19):6212-7. doi: 10.1016/j.bmcl.2012.08.020. Epub 2012 Aug 10.

Synthesis and optimization of substituted furo[2,3-d]-pyrimidin-4-amines and 7H-pyrrolo[2,3-d]pyrimidin-4-amines as ACK1 inhibitors.

Author information

1
Department of Medicinal Chemistry, Amgen Inc., 1120 Veterans Blvd., South San Francisco, CA 94080, USA. xjiao@amgen.com

Abstract

Two classes of ACK1 inhibitors, 4,5,6-trisubstituted furo[2,3-d]pyrimidin4-amines and 4,5,6-trisubstituted 7H-pyrrolo[2,3-d]pyrimidin-4-amines, were discovered and evaluated as ACK1 inhibitors. Further structural refinement led to the identification of potent and selective dithiolane inhibitor 37.

PMID:
22929232
DOI:
10.1016/j.bmcl.2012.08.020
[Indexed for MEDLINE]

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