Modification of cap group in δ-lactam-based histone deacetylase (HDAC) inhibitors

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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 LeeJong 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
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