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Title 

Structure and property based design, synthesis and biological evaluation of γ-lactam based HDAC inhibitors: Part II

Authors 

C LeeE ChoiM ChoB LeeSoo Jin OhS K ParkK LeeH M KimG Han

Publisher 

Elsevier

Issue Date 

2012

Citation 

Bioorganic & Medicinal Chemistry Letters, vol. 22, no. 12, pp. 4189-4192

Keywords 

DockingHistone deacetylasesInhibitorOptimizationProperty

Abstract 

Histone deacetylases (HDACs) are involved in post-translational modification and epi-genetic expression, and have been the intriguing targets for treatment of cancer. In previous study, we reported synthesis and the biological preliminary results of γ-lactam based HDAC inhibitors. Based on the previous results, smaller γ-lactam core HDAC inhibitors are more active than the corresponding series of larger δ-lactam based analogues and the hydrophobic and bulky cap groups are required for better potency which decreased microsomal stability. Thus, γ-lactam analogues with methoxy, trifluoromethyl groups of ortho-, meta-, para-positions of cap group were prepared and evaluated their biological potency. Among them, trifluoromethyl analogues, which have larger lipophilicity, showed better HDAC inhibitory activity than other analogues. In overall, lipophilicity leads to increase hydrophobic interaction between surface of HDAC active site and HDAC inhibitor, improves HDAC inhibitory activity.

ISSN 

0960-894X

Link 

http://dx.doi.org/10.1016/j.bmcl.2012.04.045

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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