高效合成SK-658及其类似物作为强效组蛋白去乙酰化酶抑制剂。
An efficient synthesis of SK-658 and its analogs as potent histone deacetylase inhibitors.
作者信息
Shahidul Islam Md, Nurul Islam Md, Ashraful Hoque Md, Nishino Norikazu, Kato Tamaki, Kim Hyun-Jung, Ito Akihiro, Yoshida Minoru
机构信息
Graduate School of Life Science and Systems Engineering, Kyushu Institute of Technology, Kitakyushu 808-0196, Japan; Department of Chemistry, Faculty of Science, University of Rajshahi, Rajshahi 6205, Bangladesh.
Graduate School of Life Science and Systems Engineering, Kyushu Institute of Technology, Kitakyushu 808-0196, Japan; Department of Chemistry, Faculty of Science, University of Rajshahi, Rajshahi 6205, Bangladesh.
出版信息
Bioorg Chem. 2015 Apr;59:145-50. doi: 10.1016/j.bioorg.2015.02.009. Epub 2015 Mar 7.
SK-658 is a potent histone deacetylase (HDAC) inhibitor that showed higher activity than SAHA due to the presence of extended hydrophobic group. We designed and synthesized thioester and SS-hybrid bearing SK-658 analogs as HDAC inhibitors. All the compounds were active in nano molar range and showed higher inhibitory activity than SAHA and SK-658. Among these, disulfide compounds showed the highest activity.
SK-658是一种强效组蛋白去乙酰化酶（HDAC）抑制剂，由于存在延伸的疏水基团，其活性高于SAHA。我们设计并合成了带有SK-658类似物的硫酯和SS杂化物作为HDAC抑制剂。所有化合物在纳摩尔范围内均具有活性，且显示出比SAHA和SK-658更高的抑制活性。其中，二硫键化合物表现出最高的活性。
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