Literature DB >> 20634068

Discovery and optimization of pyrazoline compounds as B-Raf inhibitors.

Matthew O Duffey1, Ruth Adams, Christopher Blackburn, Ryan W Chau, Susan Chen, Katherine M Galvin, Khristofer Garcia, Alexandra E Gould, Paul D Greenspan, Sean Harrison, Shih-Chung Huang, Mi-Sook Kim, Bheemashankar Kulkarni, Steven Langston, Jane X Liu, Li-Ting Ma, Saurabh Menon, Masayuki Nagayoshi, R Scott Rowland, Tricia J Vos, Tianlin Xu, Johnny J Yang, Shaoxia Yu, Qin Zhang.   

Abstract

The discovery of novel pyrazoline derivatives as B-Raf (V600E) inhibitors is described in this report. Chemical modification of the pyrazoline scaffold led to the development of SAR and identified potent and selective inhibitors of B-Raf (V600E). Determination of the pharmacokinetic properties of selected inhibitors is also reported. 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 20634068     DOI: 10.1016/j.bmcl.2010.06.113

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


  2 in total

1.  Identification and synthesis of N-(thiophen-2-yl) benzamide derivatives as BRAF(V600E) inhibitors.

Authors:  Yunfeng Xie; Xianjie Chen; Jie Qin; Xiangqian Kong; Fei Ye; Yuren Jiang; Hong Liu; Hualiang Jiang; Ronen Marmorstein; Cheng Luo
Journal:  Bioorg Med Chem Lett       Date:  2013-02-26       Impact factor: 2.823

2.  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
  2 in total

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