Literature DB >> 21536432

Non-oxime pyrazole based inhibitors of B-Raf kinase.

Bradley J Newhouse1, Joshua D Hansen, Jonas Grina, Mike Welch, George Topalov, Nicole Littman, Michele Callejo, Matthew Martinson, Sarah Galbraith, Ellen R Laird, Barbara J Brandhuber, Guy Vigers, Tony Morales, Rich Woessner, Nikole Randolph, Joseph Lyssikatos, Alan Olivero.   

Abstract

The synthesis and biological evaluation of non-oxime pyrazole based B-Raf inhibitors is reported. Several oxime replacements have been prepared and have shown excellent enzyme activity. Further optimization of fused pyrazole 2a led to compound 38, a selective and potent B-Raf inhibitor.
Copyright © 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 21536432     DOI: 10.1016/j.bmcl.2010.12.038

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


  5 in total

Review 1.  Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review.

Authors:  Khalid Karrouchi; Smaail Radi; Youssef Ramli; Jamal Taoufik; Yahia N Mabkhot; Faiz A Al-Aizari; M'hammed Ansar
Journal:  Molecules       Date:  2018-01-12       Impact factor: 4.411

2.  Molecular modeling, dynamics simulations, and binding efficiency of berberine derivatives: A new group of RAF inhibitors for cancer treatment.

Authors:  Parham Jabbarzadeh Kaboli; Patimah Ismail; King-Hwa Ling
Journal:  PLoS One       Date:  2018-03-22       Impact factor: 3.240

3.  Design, synthesis, anticancer evaluation and docking studies of novel 2-(1-isonicotinoyl-3-phenyl-1H-pyrazol-4-yl)-3-phenylthiazolidin-4-one derivatives as Aurora-A kinase inhibitors.

Authors:  Meenu Beniwal; Neelam Jain; Sandeep Jain; Navidha Aggarwal
Journal:  BMC Chem       Date:  2022-08-17

4.  Small molecule induced reactivation of mutant p53 in cancer cells.

Authors:  Xiangrui Liu; Rainer Wilcken; Andreas C Joerger; Irina S Chuckowree; Jahangir Amin; John Spencer; Alan R Fersht
Journal:  Nucleic Acids Res       Date:  2013-04-29       Impact factor: 16.971

5.  Modification, biological evaluation and 3D QSAR studies of novel 2-(1,3-diaryl- 4,5-dihydro-1H-pyrazol-5-yl)phenol derivatives as inhibitors of B-Raf kinase.

Authors:  Yu-Shun Yang; Fei Zhang; Dan-Jie Tang; Yong-Hua Yang; Hai-Liang Zhu
Journal:  PLoS One       Date:  2014-05-14       Impact factor: 3.240

  5 in total

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