Literature DB >> 18662874

Knowledge-based design of 7-azaindoles as selective B-Raf inhibitors.

Jun Tang1, Toshihiro Hamajima, Masato Nakano, Hideyuki Sato, Scott H Dickerson, Karen E Lackey.   

Abstract

The synthesis of a 7-azaindole series of novel, potent B-Raf kinase inhibitors using knowledge-based design was carried out. Compound 6h exhibits not only excellent potency in both the enzyme assay (IC(50)=2.5 nM) and the cellular assay (IC(50)=63 nM), but also has an outstanding selectivity profile against other kinases.

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Year:  2008        PMID: 18662874     DOI: 10.1016/j.bmcl.2008.07.019

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


  4 in total

1.  Pyrazolopyridine Inhibitors of B-Raf(V600E). Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors.

Authors:  Steve Wenglowsky; Li Ren; Kateri A Ahrendt; Ellen R Laird; Ignacio Aliagas; Bruno Alicke; Alex J Buckmelter; Edna F Choo; Victoria Dinkel; Bainian Feng; Susan L Gloor; Stephen E Gould; Stefan Gross; Janet Gunzner-Toste; Joshua D Hansen; Georgia Hatzivassiliou; Bonnie Liu; Kim Malesky; Simon Mathieu; Brad Newhouse; Nicholas J Raddatz; Yingqing Ran; Sumeet Rana; Nikole Randolph; Tyler Risom; Joachim Rudolph; Scott Savage; LeAnn T Selby; Michael Shrag; Kyung Song; Hillary L Sturgis; Walter C Voegtli; Zhaoyang Wen; Brandon S Willis; Richard D Woessner; Wen-I Wu; Wendy B Young; Jonas Grina
Journal:  ACS Med Chem Lett       Date:  2011-03-08       Impact factor: 4.345

2.  Scope and limitations of a DMF bio-alternative within Sonogashira cross-coupling and Cacchi-type annulation.

Authors:  Kirsty L Wilson; Alan R Kennedy; Jane Murray; Ben Greatrex; Craig Jamieson; Allan J B Watson
Journal:  Beilstein J Org Chem       Date:  2016-09-08       Impact factor: 2.883

Review 3.  The azaindole framework in the design of kinase inhibitors.

Authors:  Jean-Yves Mérour; Frédéric Buron; Karen Plé; Pascal Bonnet; Sylvain Routier
Journal:  Molecules       Date:  2014-11-28       Impact factor: 4.411

4.  Solvent-Free C-3 Coupling of Azaindoles with Cyclic Imines.

Authors:  Khadija Belasri; Ferenc Fülöp; István Szatmári
Journal:  Molecules       Date:  2019-10-04       Impact factor: 4.411

  4 in total

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