Powered by OpenAIRE graph
image/svg+xml Jakob Voss, based on art designer at PLoS, modified by Wikipedia users Nina and Beao Closed Access logo, derived from PLoS Open Access logo. This version with transparent background. http://commons.wikimedia.org/wiki/File:Closed_Access_logo_transparent.svg Jakob Voss, based on art designer at PLoS, modified by Wikipedia users Nina and Beao Bioorganic & Medicin...arrow_drop_down
image/svg+xml Jakob Voss, based on art designer at PLoS, modified by Wikipedia users Nina and Beao Closed Access logo, derived from PLoS Open Access logo. This version with transparent background. http://commons.wikimedia.org/wiki/File:Closed_Access_logo_transparent.svg Jakob Voss, based on art designer at PLoS, modified by Wikipedia users Nina and Beao
Bioorganic & Medicinal Chemistry Letters
Article . 2011 . Peer-reviewed
License: Elsevier TDM
Data sources: Crossref
https://pubmed.ncbi.nlm.nih.go...
Article . 2011
Data sources: Europe PubMed Central
https://dx.doi.org/10.1016/j.b...
Article
Data sources: Microsoft Academic Graph
 View all 2 versions

Discovery and SAR of spirochromane Akt inhibitors

descriptionPublicationkeyboard_double_arrow_right Article 01 Apr 2011 English Publisher:Elsevier BVJournal:Bioorganic & Medicinal Chemistry Letters, volume 21, pages 2,410-2,414 (issn: 0960-894X, Copyright policy )
Authors: Nicholas C, Kallan; Keith L, Spencer; James F, Blake; Rui, Xu; Justin, Heizer; Josef R, Bencsik; Ian S, Mitchell; +9 Authors

doi: 10.1016/j.bmcl.2011.02.073

pmid: 21392984

Discovery and SAR of spirochromane Akt inhibitors

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.

Related Organizations
Keywords

Structure-Activity Relationship, Binding Sites, Drug Evaluation, Preclinical, Crystallography, X-Ray, Protein Kinase Inhibitors, Proto-Oncogene Proteins c-akt

  • BIP!
    Impact byBIP!
    citations
    This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
    		 35
    popularity
    This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
    		 Top 10%
    influence
    This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
    		 Top 10%
    impulse
    This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
    		 Top 10%
Powered by OpenAIRE graph
citations
This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Citations provided by BIP!
popularity
This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
BIP!Popularity provided by BIP!
influence
This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Influence provided by BIP!
impulse
This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
BIP!Impulse provided by BIP!
35
Top 10%
Top 10%
Top 10%