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Yu, Wei-Chieh; Yeh, Tsung-Yu; Ye, Chih-Hung; Chong, Patrick Chun Theng; Ho, Yi-Hsun; So, Dorothy Kazuno; Yap, Kah Yi; Peng, Guan-Ru; Shao, Chi-Hsuan; Jagtap, Ajit Dhananjay; Chern, Ji-Wang; Lin, Chen-Si; Lin, Shau-Ping; Lin, Shuei-Liong; Yu, Shu-Han; Yu, Chao-Wu
Journal of medicinal chemistry, 08/2023, Volume: 66, Issue: 15Journal Article
Idiopathic pulmonary fibrosis is incurable, and its progression is difficult to control and thus can lead to pulmonary deterioration. Pan-histone deacetylase inhibitors such as SAHA have shown potential for modulating pulmonary fibrosis yet with off-target effects. Therefore, selective HDAC inhibitors would be beneficial for reducing side effects. Toward this goal, we designed and synthesized 24 novel HDAC6, HDAC8, or dual HDAC6/8 inhibitors and established a two-stage screening platform to rapidly screen for HDAC inhibitors that effectively mitigate TGF-β-induced pulmonary fibrosis. The first stage consisted of a mouse NIH-3T3 fibroblast prescreen and yielded five hits. In the second stage, human pulmonary fibroblasts (HPFs) were used, and four out of the five hits were tested for caco-2 permeability and liver microsome stability to give two potential leads: J27644 (15) and 20. This novel two-stage screen platform will accelerate the discovery and reduce the cost of developing HDAC inhibitors to mitigate TGF-β-induced pulmonary fibrosis.
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