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Title 

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

Authors 

Hwan Mook KimKiho LeeB W ParkDong Kyu RyuKangjeon KimChang Woo LeeSong Kyu ParkJ W HanH Y LeeG Han

Publisher 

Elsevier

Issue Date 

2006

Citation 

Bioorganic & Medicinal Chemistry Letters, vol. 16, no. 15, pp. 4068-4070

Keywords 

δ-Lactamanticancerhistone deacetylasering closure metathesishistone deacetylase inhibitorlactam derivativecancer inhibitioncell growthdrug synthesisenzyme inhibition

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.

ISSN 

0960-894X

Link 

http://dx.doi.org/10.1016/j.bmcl.2006.04.091

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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