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- Title
- Modification of cap group in δ-lactam-based histone deacetylase (HDAC) inhibitors
- Author(s)
- Hwan Mook Kim; S H Hong; M S Kim; Chang Woo Lee; Jong Soon Kang; Kiho Lee; Song Kyu Park; J W Han; H Y Lee; Y Choi; H J Kwon; G Han
- Bibliographic Citation
- Bioorganic & Medicinal Chemistry Letters, vol. 17, no. 22, pp. 6234-6238
- Publication Year
- 2007
- Abstract
- Novel δ-lactam-based HDAC inhibitors which have various substituted benzyl, bi-aromatic cap groups were prepared using ring closure metathesis reaction, and evaluated their HDAC inhibitory activities and anti-proliferative effects. Among prepared analogues, 11m and 11o have very strong HDAC enzymatic inhibition and showed the most potent growth inhibitory activity to five human tumor cell lines including PC-3, ACHN, NUGC-3, HCT-15, and MBA-MB-231 tumor cell lines. Compounds 11m and 11o also showed good tumor growth inhibition of MDA-MB-231 cells in in vivo xenograft model. Structure-activity relationship study using docking model explained the significance of hydrophobic aromatic cap groups for their in vitro activities.
- Keyword
- In vivo xenograft modelAnticancer chemotherapyDocking modelEnzyme inhibitorGrowth inhibitionHDACHistone deacetylase
- ISSN
- 0960-894X
- Publisher
- Elsevier
- DOI
- http://dx.doi.org/10.1016/j.bmcl.2007.09.034
- Type
- Article
- Appears in Collections:
- Ochang Branch Institute > Division of National Bio-Infrastructure > Laboratory Animal Resource & Research Center > 1. Journal Articles
- Files in This Item:
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