Literature DB >> 14698170

A novel series of potent and selective IKK2 inhibitors.

Alistair H Bingham1, Richard J Davenport, Lewis Gowers, Roland L Knight, Christopher Lowe, David A Owen, David M Parry, Will R Pitt.   

Abstract

A novel series of aminopyrimidine IKK2 inhibitors have been developed which show excellent in vitro inhibition of this enzyme and good selectivity over the IKK1 isoform. The relative potency and selectivity of these compounds has been rationalized using QSAR and structure-based modelling.

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Year:  2004        PMID: 14698170     DOI: 10.1016/j.bmcl.2003.10.047

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  8 in total

Review 1.  A medicinal chemist's guide to molecular interactions.

Authors:  Caterina Bissantz; Bernd Kuhn; Martin Stahl
Journal:  J Med Chem       Date:  2010-07-22       Impact factor: 7.446

Review 2.  NF-κB signaling and bone resorption.

Authors:  Y Abu-Amer
Journal:  Osteoporos Int       Date:  2013-03-07       Impact factor: 4.507

3.  IKKβ inhibitor identification: a multi-filter driven novel scaffold.

Authors:  Shanthi Nagarajan; Hyunah Choo; Yong Seo Cho; Kye Jung Shin; Kwang-Seok Oh; Byung Ho Lee; Ae Nim Pae
Journal:  BMC Bioinformatics       Date:  2010-10-15       Impact factor: 3.169

4.  Discovery of a novel IKK-β inhibitor by ligand-based virtual screening techniques.

Authors:  Stefan M Noha; Atanas G Atanasov; Daniela Schuster; Patrick Markt; Nanang Fakhrudin; Elke H Heiss; Olivia Schrammel; Judith M Rollinger; Hermann Stuppner; Verena M Dirsch; Gerhard Wolber
Journal:  Bioorg Med Chem Lett       Date:  2010-10-20       Impact factor: 2.823

5.  Identification of human IKK-2 inhibitors of natural origin (part I): modeling of the IKK-2 kinase domain, virtual screening and activity assays.

Authors:  Esther Sala; Laura Guasch; Justyna Iwaszkiewicz; Miquel Mulero; Maria-Josepa Salvadó; Montserrat Pinent; Vincent Zoete; Aurélien Grosdidier; Santiago Garcia-Vallvé; Olivier Michielin; Gerard Pujadas
Journal:  PLoS One       Date:  2011-02-24       Impact factor: 3.240

Review 6.  IRAK-4 inhibitors for inflammation.

Authors:  Zhulun Wang; Holger Wesche; Tracey Stevens; Nigel Walker; Wen-Chen Yeh
Journal:  Curr Top Med Chem       Date:  2009       Impact factor: 3.295

7.  Kinase inhibitors for the treatment of inflammatory and autoimmune disorders.

Authors:  Shripad S Bhagwat
Journal:  Purinergic Signal       Date:  2008-06-21       Impact factor: 3.765

8.  Synthesis and profiling of a 3-aminopyridin-2-one-based kinase targeted fragment library: Identification of 3-amino-5-(pyridin-4-yl)pyridin-2(1H)-one scaffold for monopolar spindle 1 (MPS1) and Aurora kinases inhibition.

Authors:  Daren Fearon; Isaac M Westwood; Rob L M van Montfort; Richard Bayliss; Keith Jones; Vassilios Bavetsias
Journal:  Bioorg Med Chem       Date:  2018-04-17       Impact factor: 3.641

  8 in total

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