Design, synthesis and activity evaluation of indole-based double – Branched HDAC1 inhibitors. Issue 8 (15th April 2019)

• Record Type: Journal Article
• Authors: Zhang, Qiuqiong; Lv, Jiahui; He, Feng; Yu, Chenggong; Qu, Ying; Zhang, Xiangna; Xu, Ana; Wu, Jingde
• Is Part Of: Bioorganic & medicinal chemistry. Volume 27:Issue 8(2019)
• Page Start: 1595
• Page End: 1604
• Publication Date: 2019-04-15
• Subjects: HDAC inhibitors -- Antiproliferative activity -- Selectivity -- Molecular docking; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; Chemistry, Clinical -- Periodicals; Chemistry, Organic -- Periodicals; Chimie bio-organique -- Périodiques; Chimie pharmaceutique -- Périodiques; 615.19
• DOI: 10.1016/j.bmc.2019.03.008
• Languages: English
• ISSNs: 0968-0896

Abstract

Graphical abstract: Abstract: Histone deacetylases inhibitors (HDACIs) represents effective treatments for cancer. In continuing our efforts to develop novel and potent HDACIs, a series of N -hydroxycinnamamide-based HDACIs with aromatic ring and various aliphatic linker have been successfully designed and synthesized. Biological evaluations established that compounds4h, 4i, 4j, 4l, 4r showed superior inhibition on histone deacetylase and antiproliferative activity in some solid tumor cell lines [HeLa, SK- N -BE(2), PC-3] compared to the known inhibitor SAHA. Among these analogs, 4l exhibited selectivity to HDAC1.