2-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase

Hsueh Yun Lee, Chih Yi Chang, Chih Jou Su, Han Li Huang, Samir Mehndiratta, Yuh Hsuan Chao, Chia Ming Hsu, Sunil Kumar, Ting Yi Sung, Yi Zhen Huang, Yu Hsuan Li, Chia Ron Yang, Jing Ping Liou

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25 Citations (Scopus)


This study reports the design and synthesis of 2-(phenylsulfonyl)quinoline N-hydroxyacrylamides (8a–k). Structure-activity relationship studies focusing on regio-effect of N-hydroxyacrylamide moiety and influence of the sulfonyl linker revealed that N-hydroxy-3-[3-(quinoline-2-sulfonyl)-phenyl]-acrylamide (8f) showed remarkable enzymatic and cellular activity. The GI50 values of 8f for HL-60, HCT116, PC-3, and A549 cells were found to be 0.29, 0.08, 0.15, and 0.27 μM, respectively. The compounds are therefore more potent than FDA approved PXD-101 and SAHA. They also have an effect on the acetylation degree of histone H3 and α-tubulin. In in vivo studies, 8f showed marked inhibition of the growth of HCT116 xenografts.

Original languageEnglish
Pages (from-to)92-101
Number of pages10
JournalEuropean Journal of Medicinal Chemistry
Publication statusPublished - Oct 21 2016


  • 2-(Phenylsulfonyl)quinoline
  • Anticancer agents
  • Histone deacetylase inhibitors

ASJC Scopus subject areas

  • Drug Discovery
  • Organic Chemistry
  • Pharmacology


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