Yingjie Zhang - Design, synthesis and biological evaluation of tyrosine-based hydroxamic acid analogs as novel histone deacetylases (HDACs) inhibitors.

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  Publication Details (including relevant citation   information):

  Bioorg.   Med. Chem.,  2011,  19  (15),   4437-4444.


  Histone   deacetylases (HDACs) are a promising target for treating cancer   and some other disorders. Herein, based on the structure of our   previously reported tetrahydroisoquinoline-based hydroxamic   acids, a novel series of tyrosine-based hydroxamic acid   derivatives was designed and synthesized as HDACs inhibitors.   Compared with tetrahydroisoquinoline-based hydroxamic acids,   tyrosine-based hydroxamic acid derivatives exhibited more potent   HDAC8 inhibitory activity. However, the antiproliferative   activities and HeLa cell nuclear extract inhibition of several   selected tyrosine-based hydroxamic acids were moderate.

  Address (URL): http://www.sciencedirect.com/science/article/pii/S096808961100486X