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Browsing by Author Han, sang - Bae

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  • Novel 3-substituted-2-oxoindoline-based N-hydroxypropenamides as Histone Deacetylase Inhibitors and Antitumor Agents

    • Authors: Do, T. M. Dung; Phan, T. P. Dung; Dao, T. K. Oanh; Pham, T. Hai; Le, T. T. Huong; Vu, D. Loi; Hahn, Huynggu; Han, Byung W.; Kim, Jisung; Han, sang - Bae; Nguyen, Hai Nam (2015)

  • Histone deacetylases (HDAC) are currently a group of validated targets for anticancer drug discovery and development. In our research program to find novel small molecules targeting these enzymes, we designed and synthesized two series of 3-hydroxyimino-2-oxoindoline- and 3- methoxyimino-2-oxoindoline-based N-hydroxypropenamides (3a-g, 6a-g). The results show that these propenamides potently inhibited HDAC2 with IC50 values in sub-micromolar range, approximately 10-fold lower than that of SAHA (also known as suberoylanilohydroxamic acid). Evaluation of cytotoxicity of these compounds in three human cancer cell lines revealed that most of the synthesized compounds were up to 5-fold mor...

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Browsing by Author Han, sang - Bae

Jump to: 0-9 A B C D E F G H I J K L M N O P Q R S T U V W X Y Z
or enter first few letters:  
Showing results 1 to 1 of 1
  • 1. Loi QT.pdf.jpg
  • Article

  • Novel 3-substituted-2-oxoindoline-based N-hydroxypropenamides as Histone Deacetylase Inhibitors and Antitumor Agents

    • Authors: Do, T. M. Dung; Phan, T. P. Dung; Dao, T. K. Oanh; Pham, T. Hai; Le, T. T. Huong; Vu, D. Loi; Hahn, Huynggu; Han, Byung W.; Kim, Jisung; Han, sang - Bae; Nguyen, Hai Nam (2015)

  • Histone deacetylases (HDAC) are currently a group of validated targets for anticancer drug discovery and development. In our research program to find novel small molecules targeting these enzymes, we designed and synthesized two series of 3-hydroxyimino-2-oxoindoline- and 3- methoxyimino-2-oxoindoline-based N-hydroxypropenamides (3a-g, 6a-g). The results show that these propenamides potently inhibited HDAC2 with IC50 values in sub-micromolar range, approximately 10-fold lower than that of SAHA (also known as suberoylanilohydroxamic acid). Evaluation of cytotoxicity of these compounds in three human cancer cell lines revealed that most of the synthesized compounds were up to 5-fold mor...