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Title 

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

Authors 

Hwan Mook KimS H HongM S KimChang Woo LeeJong Soon KangKiho LeeSong Kyu ParkJ W HanH Y LeeY ChoiH J KwonG Han

Publisher 

Elsevier

Issue Date 

2007

Citation 

Bioorganic & Medicinal Chemistry Letters, vol. 17, no. 22, pp. 6234-6238

Keywords 

anticancer chemotherapydocking modelenzyme inhibitorgrowth inhibitionHDAChistone deacetylasein vivo xenograft modelhistone deacetylase inhibitorlactam derivativechemical modification

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.

ISSN 

0960-894X

Link 

http://doi.org/10.1016/j.bmcl.2007.09.034

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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