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Discovery of Pyridone-Based Histone Deacetylase Inhibitors: Approaches for Metabolic Stability

✍ Scribed by Cho, Misun; Choi, Eunhyun; Yang, Jee Sun; Lee, Chulho; Seo, Jeong Jea; Kim, Beom Seok; Oh, Soo Jin; Kim, Hwan Mook; Lee, Kiho; Park, Song-Kyu; Kwon, Ho Jeong; Han, Gyoonhee


Book ID
118231563
Publisher
John Wiley and Sons
Year
2013
Tongue
English
Weight
570 KB
Volume
8
Category
Article
ISSN
1860-7179

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The novel d-lactam based HDAC inhibitor, KBH-A118 (3) shows a good HDAC enzyme and cancer cell growth inhibitory activities but has undesirable pharmacokinetics profiles because of instability in mouse liver microsome. To improve metabolic stability, various analogues were prepared with substituents