Design, synthesis and biological evaluation of novel histone deacetylase (HDAC) inhibitors derived from β-elemene scaffold

• Main Authors: Yuan Gao (Author), Jilong Duan (Author), Xiawen Dang (Author), Yinghui Yuan (Author), Yu Wang (Author), Xingrui He (Author), Renren Bai (Author), Xiang-Yang Ye (Author), Tian Xie (Author)
• Format: Book
• Published: Taylor & Francis Group, 2023-12-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

β-Elemene is the major active ingredient of TCM anticancer drug elemene extracts. To further improve its antitumor activity and poor solubility, a polar HDACi pharmacophore was incorporated its scaffold. Systematic SAR studies led to the discovery of compounds 27f and 39f, which exhibited potent inh...