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Property-Based Optimization of Hydroxamate-Based γ-Lactam HDAC Inhibitors to Improve Their Metabolic Stability and Pharmacokinetic Profiles

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

Book ID: 118062387
Publisher: American Chemical Society
Year: 2012
Tongue: English
Weight: 619 KB
Volume: 55
Category: Article
ISSN: 0022-2623
DOI: 10.1021/jm3009376

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Property based optimization of δ-lactam

Property based optimization of δ-lactam HDAC inhibitors for metabolic stability

✍ Hong Chul Yoon; Eunhyun Choi; Jung Eun Park; Misun Cho; Jeong Jea Seo; Soo Jin O 📂 Article 📅 2010 🏛 Elsevier Science 🌐 English ⚖ 205 KB

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