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Design, synthesis, and preliminary bioactivity evaluation of N ‐benzylpyrimidin‐2‐amine derivatives as novel histone deacetylase inhibitor
Author(s) -
Zhou Yi,
Dun Yanyan,
Fu Huansheng,
Wang Lei,
Pan Xiaole,
Yang Xinying,
Fang Hao
Publication year - 2017
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.13019
Subject(s) - histone deacetylase , chemistry , inhibitory postsynaptic potential , in vitro , amine gas treating , biochemistry , histone , enzyme , histone deacetylase inhibitor , hdac11 , histone deacetylase 5 , stereochemistry , pharmacology , biology , organic chemistry , dna , neuroscience
Histone deacetylase (HDAC) inhibitors have been identified for the treatment of cancer. Lately, we designed and synthesized a series of substituted N ‐benzylpyrimidin‐2‐amine derivatives as potent HDAC inhibitors. In vitro HDAC inhibitory activities and antiproliferative activities of target compounds were investigated. Some target compounds showed potent HDAC inhibitory activities and possessed obvious antiproliferative activity against tumor cells. Target compounds 6a , 6d , 8a , 8c, and 8f not only exhibited almost equally enzymatic inhibitory activity with SAHA , but showed better antiproliferative activities.