2. Academic Validation
  3. Structure-activity relationship studies of a series of novel delta-lactam-based histone deacetylase inhibitors

Structure-activity relationship studies of a series of novel delta-lactam-based histone deacetylase inhibitors

  • J Med Chem. 2007 May 31;50(11):2737-41. doi: 10.1021/jm0613828.
Hwan Mook Kim 1,  Dong-Kyu Ryu,  Yongseok Choi,  Bum Woo Park,  Kiho Lee,  Sang Bae Han,  Chang-Woo Lee,  Moo-Rim Kang,  Jong Soon Kang,  Shanthaveerappa K Boovanahalli,  Song-Kyu Park,  Jung Whan Han,  Tae-Gyu Chun,  Hee-Yoon Lee,  Ky-Youb Nam,  Eun Hyun Choi,  Gyoonhee Han
Affiliations

Affiliation

  • 1 Bioevaluation Center, KRIBB, Daejeon 305-806, Korea.
PMID: 17477518 DOI: 10.1021/jm0613828
Abstract

We synthesized a series of delta-lactam-based HDAC inhibitors that were identified with various degrees of anti-inflammatory and cell growth inhibitory activities. Compounds possessing significant HDAC inhibitory activity exhibited both anti-inflammatory and cell growth inhibitory activities as well as significant tumor growth inhibition in the in vivo tumor xenograft experiments. Besides, these compounds demonstrated anti-inflammatory properties in vitro via suppression of the production of the proinflammatory cytokine TNF-alpha and nitric oxide by LPS-stimulated RAW264.7 cells.

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