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Updated: Jul 15, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Structure-activity relationship studies of a series of novel delta-lactam-based histone deacetylase inhibitors
Hwan Mook Kim1, Dong-Kyu Ryu, Yongseok Choi
1Bioevaluation Center, KRIBB, Daejeon 305-806, Korea.
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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