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Title 

Synthesis, bioevaluation and docking study of 5-substitutedphenyl-1,3,4-thiadiazole-based hydroxamic acids as histone deacetylase inhibitors and antitumor agents

Authors 

N H NamT L HuongD T M DungP T P DungD T K OanhS H ParkK KimB W HanJi Eun YunJong Soon KangY KimS B Han

Publisher 

Informa Healthcare

Issue Date 

2014

Citation 

Journal of Enzyme Inhibition and Medicinal Chemistry, vol. 29, no. 5, pp. 611-618

Keywords 

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

Abstract 

Since the first histone deacetylase (HDAC) inhibitor (Zolinza®, widely known as suberoylanilide hydroxamic acid; SAHA) was approved by the Food and Drug Administration for the treatment of T-cell lymphoma in 2006, the search for newer HDAC inhibitors has attracted a great deal of interest of medicinal chemists worldwide. As a continuity of our ongoing research in this area, we designed and synthesized a series of 5-substitutedphenyl-1,3,4-thiadiazole-based hydroxamic acids as analogues of SAHA and evaluated their biological activities. A number of compounds in this series, for example, N1-hydroxy-N8-(5-(2-chlorophenyl)-1,3,4-thiadiazol-2-yl)octandiamide (5b), N1-hydroxy-N8-(5-(3-chlorophenyl-1,3,4-thiadiazol-2-yl)octandiamide (5c) and N1-hydroxy-N8-(5-(4-chlorophenyl)-1,3,4-thiadiazol-2-yl)octandiamide (5d), were found to possess potent anticancer cytotoxicity and HDAC inhibition effects. Compounds 5b-d were generally two- to five-fold more potent in terms of cytotoxicity compared to SAHA against five cancer cell lines tested. Docking studies revealed that these hydroxamic acid displayed higher affinities than SAHA toward HDAC8

ISSN 

1475-6366

Link 

http://dx.doi.org/10.3109/14756366.2013.832238

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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