Construction and screening of solution-phase derived library of fenbufen and ethacrynic acid

A process for synthesizing and screening solution phase derived libraries of fenbufen and ethacrynic acid is provided in the present invention. Compounds in the present invention having cytotoxicities are useful for a variety of therapeutic applications.

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Main Authors Yu, Chung-Shan, Su, Yuan-Hsiao, Chiang, Li-Wu, Chen, Chia-Rong, Chen, Shao-Wei, Huang, Chia-Wen, Huang, Ho-Lien, Huang, Yin-Cheng
Format Patent
LanguageEnglish
Published 10.01.2012
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Abstract A process for synthesizing and screening solution phase derived libraries of fenbufen and ethacrynic acid is provided in the present invention. Compounds in the present invention having cytotoxicities are useful for a variety of therapeutic applications.
AbstractList A process for synthesizing and screening solution phase derived libraries of fenbufen and ethacrynic acid is provided in the present invention. Compounds in the present invention having cytotoxicities are useful for a variety of therapeutic applications.
Author Su, Yuan-Hsiao
Chiang, Li-Wu
Huang, Yin-Cheng
Chen, Shao-Wei
Chen, Chia-Rong
Yu, Chung-Shan
Huang, Chia-Wen
Huang, Ho-Lien
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– sequence: 3
  givenname: Li-Wu
  surname: Chiang
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  surname: Chen
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  fullname: Huang, Chia-Wen
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  givenname: Ho-Lien
  surname: Huang
  fullname: Huang, Ho-Lien
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  givenname: Yin-Cheng
  surname: Huang
  fullname: Huang, Yin-Cheng
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References Bertrand Carboni et al., Aliphatic Amino Azides as Key Building Blocks for Efficient Polyamine Syntheses, J. Org. Chem. 1993,58, 3736-3741.
Will Bannwarth et al., Multicomponent Condensations (MCCs), Combinatorial Chemistry a Practical Approach, 2000, pp. 6-21.
Subra et al. (Peptides, 2000, Proceedings of the European Peptide Symposium, 26th Montpellier, France, Sep. 10-15).
Jae Wook Lee et al., An efficient and practical method for the synthesis of mono-N-protected a,v-diaminoalkanes, Tetrahedron Letters 42 (2001) 2709-2711.
Guangyi Jin et al., Amide derivatives of ethacrynic acid: Synthesis and evaluation as antagonists of Wnt/b-catenin signaling and CLL cell survival, Bioorganic & Medicinal Chemistry Letters 19 (2009) 606-609.
Chiang, Li-Wu et al., Combining a Solution-Phase Derived Library with In-Situ Cellular Bioassay: Prompt Screening of Amide-Forming Minilibraries Using MTT Assay, Chem. Pharm. Bull., vol. 57 (7), 2009, pp. 714-718.
Rui Wang et al., Ethacrynic Acid Butyl-Ester Induces Apoptosis in Leukemia Cells through a Hydrogen Peroxide-Mediated Pathway Independent of Glutathione S-Transferase P1-1 Inhibition, Cancer Res 2007; 67: (16). Aug. 15, 2007, 7856-7864.
Phil B. Alper et al., Metal Catalyzed Diazo Transfer for the Synthesis of Azides From Amines, Tetrahedron Letters, 1996, vol. 37, No. 34, pp. 6029-6032.
Desheng Lu et al., Ethacrynic Acid Exhibits Selective Toxicity to Chronic Lymphocytic Leukemia Cells by Inhibition of the Wnt/b-Catenin Pathway, PLoS ONE, Dec. 2009, vol. 4, Issue 12, pp. 1-10.
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