244156-66-9Relevant academic research and scientific papers
Identification and Biological Evaluation of Novel Type II B-RafV600E Inhibitors
Wang, Peng-Fei,Wang, Ze-Feng,Qiu, Han-Yue,Huang, Yue,Hu, Hui-Min,Wang, Zhong-Chang,Zhu, Hai-Liang
, p. 2558 - 2566 (2018/11/23)
The mitogen-activated protein kinase (MAPK) pathway plays a vital role in signal transduction networks. Severe diseases may be triggered if it is disturbed by mutated components, especially the kinase B-RafV600E. New inhibitors of the kinase ar
SOLUBLE EPOXIDE HYDROLASE INHIBITORS FOR THE TREATMENT OF RHEUMATOID ARTHRITIS
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Page/Page column 40, (2008/12/05)
Methods for reducing autoimmune induced inflammation, including rheumatoid arthritis in a subject in need of such therapy are disclosed.
SOLUBLE EPOXIDE HYDROLASE INHIBITORS FOR TREATMENT OF METABOLIC SYNDROME AND RELATED DISORDERS
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Page/Page column 47, (2008/12/07)
Compounds, compositions, and methods for inhibiting the onset of metabolic syndrome and treating related disorders in a subject in need of such therapy are disclosed.
Synthesis and evaluation of inhibitors of transthyretin amyloid formation based on the non-steroidal anti-inflammatory drug, flufenamic acid
Baures, Paul W.,Oza, Vibha B.,Peterson, Scott A.,Kelly, Jeffery W.
, p. 1339 - 1347 (2007/10/03)
A light scattering-based amyloid fibril formation assay was employed to evaluate potential inhibitors of transthyretin (TTR) amyloid fibril formation in vitro. Twenty nine aromatic small molecules, some with homology to flufenamic acid (a known non-steroidal anti-inflammatory drug) were tested to identify important structural features for inhibitor efficacy. The results of these experiments and earlier data suggest that likely inhibitors will have aromatic-based structures with at least two aromatic rings. The ring or fused ring system occupying the outermost TTR binding pocket needs to be substituted with an acidic functional group (e.g. a carboxylic acid) to interact with complimentary charges in the TTR binding site. The promising TTR amyloid fibril inhibitors ranked in order of efficacy are: 2>4~7>3>9>6>21 (see Structural summary of the best transthyretin amyloid fibril formation inhibitors identified in this study. The order of efficacy is: 2>4~7>3>9>6>21.). Copyright (C) 1999 Elsevier Science Ltd.
