Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 28, Issue 3, Pages -Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2019.115250
Keywords
Histone deacetylase; 2-Quinolineacrylamide; Ullmann reaction
Funding
- Ministry of Science and Technology, Taiwan [MOST 105-2320-B-038-010]
- Taipei Medical University [TMU104-AE1-B17]
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A series of C6-substituted N-hydroxy-2-quinolineacrylamides (3-15), with four types of bridging groups have been synthesized. Most of these compounds exhibit antiproliferative activity against A549 and HCT116 cells and Western blot analysis revealed that they are able to inhibit HDAC. Measurement of the HDAC isoform activity of ether-containing compounds showed that compound 9 has distinct HDAC6 selectivity, more than 300-fold over other isoforms. This paper describes the development of 6-aryloxy-N-hydroxy-2-quinolineacrylamides as potential HDAC6 inhibitors.
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