Discovery and SAR of spirochromane Akt inhibitors

Nicholas C. Kallan; Keith L. Spencer; James F. Blake; Rui Xu; Justin Heizer; Josef R. Bencsik; Ian S. Mitchell; Susan L. Gloor; Matthew Martinson; Tyler Risom; Stefan D. Gross; Tony H. Morales; Wen I. Wu; Guy P.A. Vigers; Barbara J. Brandhuber; Nicholas J. Skelton

Journal Article

Discovery and SAR of spirochromane Akt inhibitors

Bioorganic and Medicinal Chemistry Letters (2011) 21(8) 2410-2414

DOI: 10.1016/j.bmcl.2011.02.073

40Citations

43Readers

Get full text

Abstract

A novel series of spirochromane pan-Akt inhibitors is reported. SAR optimization furnished compounds with improved enzyme potencies and excellent selectivity over the related AGC kinase PKA. Attempted replacement of the phenol hinge binder provided compounds with excellent Akt enzyme and cell activities but greatly diminished selectivity over PKA. © 2011 Elsevier Ltd. All rights reserved.

Author supplied keywords

Akt kinase inhibitors

Cite

CITATION STYLE

APA

Kallan, N. C., Spencer, K. L., Blake, J. F., Xu, R., Heizer, J., Bencsik, J. R., … Skelton, N. J. (2011). Discovery and SAR of spirochromane Akt inhibitors. Bioorganic and Medicinal Chemistry Letters, 21(8), 2410–2414. https://doi.org/10.1016/j.bmcl.2011.02.073

Discovery and SAR of spirochromane Akt inhibitors

Abstract

Author supplied keywords

Cite

Register to see more suggestions