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Property-Based Optimization of Hydroxamate-Based gamma-Lactam HDAC Inhibitors to Improve Their Metabolic Stability and Pharmacokinetic Profiles
- Authors
- 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
- Issue Date
- 13-Dec-2012
- Publisher
- AMER CHEMICAL SOC
- Citation
- JOURNAL OF MEDICINAL CHEMISTRY, v.55, no.23, pp.10766 - 10770
- Indexed
- SCIE
SCOPUS
- Journal Title
- JOURNAL OF MEDICINAL CHEMISTRY
- Volume
- 55
- Number
- 23
- Start Page
- 10766
- End Page
- 10770
- ISSN
- 0022-2623
- Abstract
- Hydroxamate-based HDAC inhibitors have promising anticancer activities but metabolic instability and poor pharmacokinetics leading to poor in vivo results. QSAR and PK studies of HDAC inhibitors showed that a gamma-lactam core and a modified cap group, including halo, alkyl, and alkoxy groups with various carbon chain linkers, improved HDAC inhibition and metabolic stability. The biological properties of the gamma-lactam HDAC inhibitors were evaluated; the compound designated 8f had potent anticancer activity and high oral bioavailability.
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Related Researcher
- Lee, Ki ho
- College of Pharmacy (Department of Pharmaceutical Science)