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Author (up) Nam, N.-H.; Huong, T.L.; Dung, D.T.M.; Dung, P.T.P.; Oanh, D.T.K.; Park, S.H.; Kim, K.; Han, B.W.; Yun, J.; Kang, J.S.; Kim, Y.; Han, S.-B.
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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 Type Journal Article
  Year 2013 Publication Journal of Enzyme Inhibition and Medicinal Chemistry Abbreviated Journal J Enzyme Inhib Med Chem  
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  Abstract Abstract Since the first histone deacetylase (HDAC) inhibitor (Zolinza(R), 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.  
  Address Department of Pharmaceutical Chemistry, Hanoi University of Pharmacy , Hanoi , Vietnam  
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  Language English Summary Language Original Title  
  Series Editor Series Title Abbreviated Series Title  
  Series Volume Series Issue Edition  
  ISSN 1475-6366 ISBN Medium  
  Area Expedition Conference  
  Notes PMID:24020585 Approved no  
  Call Number @ @ Serial 42260  
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