Literature DB >> 18621524

The identification of potent, selective and CNS penetrant furan-based inhibitors of B-Raf kinase.

Andrew K Takle1, Mark J Bamford, Susannah Davies, Robert P Davis, David K Dean, Alessandra Gaiba, Elaine A Irving, Frank D King, Antoinette Naylor, Christopher A Parr, Alison M Ray, Alastair D Reith, Beverley B Smith, Penelope C Staton, Jon G A Steadman, Tania O Stean, David M Wilson.   

Abstract

Modification of the potent imidazole-based B-Raf inhibitor SB-590885 resulted in the identification of a series of furan-based derivatives with enhanced CNS penetration. One such compound, SB-699393 (17), was examined in vivo to challenge the hypothesis that selective B-Raf inhibitors may be of value in the treatment of stroke.

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Year:  2008        PMID: 18621524     DOI: 10.1016/j.bmcl.2008.06.070

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


  9 in total

Review 1.  Targeting protein kinases in central nervous system disorders.

Authors:  Laura K Chico; Linda J Van Eldik; D Martin Watterson
Journal:  Nat Rev Drug Discov       Date:  2009-11       Impact factor: 84.694

2.  A combined 3D-QSAR and molecular docking strategy to understand the binding mechanism of (V600E)B-RAF inhibitors.

Authors:  Zaheer Ul-Haq; Uzma Mahmood; Sauleha Reza
Journal:  Mol Divers       Date:  2012-10-04       Impact factor: 2.943

3.  Chemical interrogation of the malaria kinome.

Authors:  Emily R Derbyshire; Vanessa Zuzarte-Luís; Andreia D Magalhães; Nobutaka Kato; Paul C Sanschagrin; Jinhua Wang; Wenjun Zhou; Chandrasekhar V Miduturu; Ralph Mazitschek; Piotr Sliz; Maria M Mota; Nathanael S Gray; Jon Clardy
Journal:  Chembiochem       Date:  2014-08-08       Impact factor: 3.164

4.  Investigation of naphthofuran moiety as potential dual inhibitor against BACE-1 and GSK-3β: molecular dynamics simulations, binding energy, and network analysis to identify first-in-class dual inhibitors against Alzheimer's disease.

Authors:  Akhil Kumar; Gaurava Srivastava; Swati Srivastava; Seema Verma; Arvind S Negi; Ashok Sharma
Journal:  J Mol Model       Date:  2017-07-24       Impact factor: 1.810

Review 5.  A guide to picking the most selective kinase inhibitor tool compounds for pharmacological validation of drug targets.

Authors:  Joost C M Uitdehaag; Folkert Verkaar; Husam Alwan; Jos de Man; Rogier C Buijsman; Guido J R Zaman
Journal:  Br J Pharmacol       Date:  2012-06       Impact factor: 8.739

6.  Structure and Reactivity of Highly Twisted N-Acylimidazoles.

Authors:  Elizabeth A Stone; Brandon Q Mercado; Scott J Miller
Journal:  Org Lett       Date:  2019-03-12       Impact factor: 6.005

7.  Novel tricyclic pyrazole BRAF inhibitors with imidazole or furan central scaffolds.

Authors:  Dan Niculescu-Duvaz; Ion Niculescu-Duvaz; Bart M J M Suijkerbuijk; Delphine Ménard; Alfonso Zambon; Arnaud Nourry; Lawrence Davies; Helen A Manne; Frank Friedlos; Lesley Ogilvie; Douglas Hedley; Andrew K Takle; David M Wilson; Jean-Francois Pons; Tom Coulter; Ruth Kirk; Neus Cantarino; Steven Whittaker; Richard Marais; Caroline J Springer
Journal:  Bioorg Med Chem       Date:  2010-06-15       Impact factor: 3.641

Review 8.  Ras/Raf/MEK/ERK and PI3K/PTEN/Akt/mTOR inhibitors: rationale and importance to inhibiting these pathways in human health.

Authors:  William H Chappell; Linda S Steelman; Jacquelyn M Long; Ruth C Kempf; Stephen L Abrams; Richard A Franklin; Jörg Bäsecke; Franca Stivala; Marco Donia; Paolo Fagone; Graziella Malaponte; Maria C Mazzarino; Ferdinando Nicoletti; Massimo Libra; Danijela Maksimovic-Ivanic; Sanja Mijatovic; Giuseppe Montalto; Melchiorre Cervello; Piotr Laidler; Michele Milella; Agostino Tafuri; Antonio Bonati; Camilla Evangelisti; Lucio Cocco; Alberto M Martelli; James A McCubrey
Journal:  Oncotarget       Date:  2011-03

9.  Site-selective Suzuki-Miyaura coupling of heteroaryl halides - understanding the trends for pharmaceutically important classes.

Authors:  Joshua Almond-Thynne; David C Blakemore; David C Pryde; Alan C Spivey
Journal:  Chem Sci       Date:  2016-08-09       Impact factor: 9.825

  9 in total

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