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Title 

5-aryl-1,3,4-thiadiazole-based hydroxamic acids as histone deacetylase inhibitors and antitumor agents: synthesis, bioevaluation and docking study

Authors 

T T L HuongD T M DungD T K OanhT T B LanP T P DungV D LoiK R KimB W HanJi Eun YunJong Soon KangY KimS B HanN H Nam

Publisher 

Bentham Science Publishers

Issue Date 

2015

Citation 

Medicinal Chemistry, vol. 11, no. 3, pp. 296-304

Keywords 

5-aryl-1,3,4-thiadiazoleCytotoxicityHeterocycleHistone deacetylase (HDAC) inhibitors

Abstract 

The search for newer histone deacetylase (HDAC) inhibitors has attracted a great deal of interest of medicinal chemists worldwide, especially after the first HDAC inhibitor (Zolinza® , widely known as SAHA or Suberoylanilide hydroxamic acid) was approved by the FDA for the treatment of Tcell lymphoma in 2006. As a continuity of our ongoing research in this area, we designed and synthesized a series of 5-aryl-1,3,4-thiadiazole-based hydroxamic acids as analogues of SAHA and evaluated their biological activities. Most of the compounds in this series, e.g. compounds with 5-aryl moiety being 2-furfuryl (5a), 5-bromofuran-2-yl (5b), 5-methylfuran-2-yl (5c), thiophen-2-yl (5d), 5-methylthiophen-2-yl (5f) and pyridyl (5g-i), were found to have potent anticancer cytotoxicity with IC50 values of generally 5-to 10-fold lower than that of SAHA in 4 human cancer cell lines assayed. Those compounds with potent cytotoxicity were also found to have strong HDAC inhibition effects. Docking studies revealed that compounds 5a and 5d displayed high affinities towards HDAC2 and 8.

ISSN 

1573-4064

Link 

http://dx.doi.org/10.2174/1573406410666140925153128

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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