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

• Autori principali: Yuan Gao (Autore), Jilong Duan (Autore), Xiawen Dang (Autore), Yinghui Yuan (Autore), Yu Wang (Autore), Xingrui He (Autore), Renren Bai (Autore), Xiang-Yang Ye (Autore), Tian Xie (Autore)
• Natura: Libro
• Pubblicazione: Taylor & Francis Group, 2023-12-01T00:00:00Z.
• Soggetti: article
• Accesso online: 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...