2. Academic Validation
  3. Synthesis and biological evaluation of 1-arylsulfonyl-5-(N-hydroxyacrylamide)indoles as potent histone deacetylase inhibitors with antitumor activity in vivo

Synthesis and biological evaluation of 1-arylsulfonyl-5-(N-hydroxyacrylamide)indoles as potent histone deacetylase inhibitors with antitumor activity in vivo

  • J Med Chem. 2012 Apr 26;55(8):3777-91. doi: 10.1021/jm300197a.
Mei-Jung Lai 1,  Han-Li Huang,  Shiow-Lin Pan,  Yi-Min Liu,  Chieh-Yu Peng,  Hsueh-Yun Lee,  Teng-Kuang Yeh,  Po-Hsien Huang,  Che-Ming Teng,  Ching-Shih Chen,  Hsun-Yueh Chuang,  Jing-Ping Liou
Affiliations

Affiliation

  • 1 School of Pharmacy, College of Pharmacy, Taipei Medical University, 250 Wuxing Street, Taipei 11031, Taiwan.
PMID: 22439863 DOI: 10.1021/jm300197a
Abstract

A series of 1-arylsulfonyl-5-(N-hydroxyacrylamide)indoles has been identified as a new class of histone deacetylase inhibitors. Compounds 8, 11, 12, 13, and 14 demonstrated stronger antiproliferative activities than 1 (SAHA) with GI(50) values ranging from 0.36 to 1.21 μM against Hep3B, MDA-MB-231, PC-3, and A549 human Cancer cell lines. Lead compound 8 showed remarkable HDAC 1, 2, and 6 isoenzymes inhibitory activities with IC(50) values of 12.3, 4.0, 1.0 nM, respectively, which are comparable to 1. In in vivo efficacy evaluation against lung A549 xenograft model, 8 displayed better antitumor activity than compound 1.

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