Synthesis, enzymatic inhibition, and cancer cell growth inhibition of novel δ-lactam-based histone deacetylase (HDAC) inhibitors

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Title
Synthesis, enzymatic inhibition, and cancer cell growth inhibition of novel δ-lactam-based histone deacetylase (HDAC) inhibitors
Author(s)
Hwan Mook Kim; Kiho Lee; B W Park; Dong Kyu Ryu; Kangjeon Kim; Chang Woo Lee; Song Kyu Park; J W Han; H Y Lee; H Y Lee; G Han
Bibliographic Citation
Bioorganic & Medicinal Chemistry Letters, vol. 16, no. 15, pp. 4068-4070
Publication Year
2006
Abstract
δ-Lactam-based hydroxamic acids, inhibitors of histone deacetylase (HDAC), have been synthesized via ring closure metathesis of key diene intermediates followed by conversion to hydroxamic acid analogues. The hydroxamic acids 12a, 12b, and 17c showed potent inhibitory activity in HDAC enzyme assay. The hydroxamic acid 12b exhibited growth inhibitory activity on five human tumor cell lines, showing good sensitivity on the MDA-MB-231 breast tumor cell.
Keyword
δ-Lactamanticancerhistone deacetylasering closure metathesis
ISSN
0960-894X
Publisher
Elsevier
DOI
http://dx.doi.org/10.1016/j.bmcl.2006.04.091
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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