An efficient synthesis of SK-658 and its analogs as potent histone deacetylase inhibitors

作者：Islam Md Shahidul; Islam Md Nurul; Hoque Md Ashraful; Nishino Norikazu; Kato Tamaki; Kim Hyun Jung; Ito Akihiro; Yoshida Minoru

来源：Bioorganic Chemistry, 2015, 59: 145-150.

DOI：10.1016/j.bioorg.2015.02.009

• Histone deacetylase inhibitor
• Zinc binding group
• SK-658 analogs
• SS-hybrid

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.

• 出版日期2015-4
• 单位RIKEN