Literature DB >> 16260133

The identification of potent and selective imidazole-based inhibitors of B-Raf kinase.

Andrew K Takle1, Murray J B Brown, Susannah Davies, David K Dean, Gerraint Francis, Alessandra Gaiba, Alex W Hird, Frank D King, Peter J Lovell, Antoinette Naylor, Alastair D Reith, Jon G Steadman, David M Wilson.   

Abstract

A novel triarylimidazole derivative, SB-590885 (33), bearing a 2,3-dihydro-1H-inden-1-one oxime substituent has been identified as a potent and extremely selective inhibitor of B-Raf kinase.

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Year:  2005        PMID: 16260133     DOI: 10.1016/j.bmcl.2005.09.072

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


  17 in total

1.  Comprehensive characterization of the Published Kinase Inhibitor Set.

Authors:  Jonathan M Elkins; Vita Fedele; Marta Szklarz; Kamal R Abdul Azeez; Eidarus Salah; Jowita Mikolajczyk; Sergei Romanov; Nikolai Sepetov; Xi-Ping Huang; Bryan L Roth; Ayman Al Haj Zen; Denis Fourches; Eugene Muratov; Alex Tropsha; Joel Morris; Beverly A Teicher; Mark Kunkel; Eric Polley; Karen E Lackey; Francis L Atkinson; John P Overington; Paul Bamborough; Susanne Müller; Daniel J Price; Timothy M Willson; David H Drewry; Stefan Knapp; William J Zuercher
Journal:  Nat Biotechnol       Date:  2015-10-26       Impact factor: 54.908

2.  BRAF signals to pro-apoptotic BIM to enhance AraC cytotoxicity induced in AML cells by Vitamin D-based differentiation agents.

Authors:  Xuening Wang; Jonathan S Harrison; George P Studzinski
Journal:  J Steroid Biochem Mol Biol       Date:  2016-09-13       Impact factor: 4.292

Review 3.  Current advances in the synthesis and biological potencies of tri- and tetra-substituted 1H-imidazoles.

Authors:  Majid M Heravi; Mansoureh Daraie; Vahideh Zadsirjan
Journal:  Mol Divers       Date:  2015-04-12       Impact factor: 2.943

4.  In situ kinase profiling reveals functionally relevant properties of native kinases.

Authors:  Matthew P Patricelli; Tyzoon K Nomanbhoy; Jiangyue Wu; Heidi Brown; David Zhou; Jianming Zhang; Subadhra Jagannathan; Arwin Aban; Eric Okerberg; Chris Herring; Brian Nordin; Helge Weissig; Qingkai Yang; Jiing-Dwan Lee; Nathanael S Gray; John W Kozarich
Journal:  Chem Biol       Date:  2011-06-24

5.  Dual Screening of BPTF and Brd4 Using Protein-Observed Fluorine NMR Uncovers New Bromodomain Probe Molecules.

Authors:  Andrew K Urick; Laura M L Hawk; Melissa K Cassel; Neeraj K Mishra; Shuai Liu; Neeta Adhikari; Wei Zhang; Camila O dos Santos; Jennifer L Hall; William C K Pomerantz
Journal:  ACS Chem Biol       Date:  2015-07-28       Impact factor: 5.100

6.  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

7.  The crystal structure of BRAF in complex with an organoruthenium inhibitor reveals a mechanism for inhibition of an active form of BRAF kinase.

Authors:  Peng Xie; Craig Streu; Jie Qin; Howard Bregman; Nicholas Pagano; Eric Meggers; Ronen Marmorstein
Journal:  Biochemistry       Date:  2009-06-16       Impact factor: 3.162

8.  Pan-Raf co-operates with PI3K-dependent signalling and critically contributes to myeloma cell survival independently of mutated RAS.

Authors:  E Müller; S Bauer; T Stühmer; A Mottok; C-J Scholz; T Steinbrunn; D Brünnert; A Brandl; H Schraud; S Kreßmann; A Beilhack; A Rosenwald; R C Bargou; M Chatterjee
Journal:  Leukemia       Date:  2016-09-30       Impact factor: 11.528

9.  Nilotinib and MEK inhibitors induce synthetic lethality through paradoxical activation of RAF in drug-resistant chronic myeloid leukemia.

Authors:  Leisl M Packer; Sareena Rana; Robert Hayward; Thomas O'Hare; Christopher A Eide; Ana Rebocho; Sonja Heidorn; Matthew S Zabriskie; Ion Niculescu-Duvaz; Brian J Druker; Caroline Springer; Richard Marais
Journal:  Cancer Cell       Date:  2011-12-13       Impact factor: 31.743

10.  The RAS/mitogen activated protein (MAP) kinase pathway in melanoma biology and therapeutics.

Authors:  Abel D Jarell; Donald Lawrence; Hensin Tsao
Journal:  Biologics       Date:  2007-12
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