Open AccessDesign, synthesis and evaluation of belinostat analogs as histone deacetylase inhibitors
Author(s) -
JieHuan Zhang,
Madhusoodanan Mottamal,
HaiShan Jin,
Shuai Guo,
Yan Gu,
Guangdi Wang,
LiMing Zhao
Publication year - 2019
Publication title -
future medicinal chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.708
H-Index - 69
eISSN - 1756-8927
pISSN - 1756-8919
DOI - 10.4155/fmc-2018-0587
Subject(s) - histone deacetylase , chemistry , in vitro , amide , pharmacology , hdac11 , biochemistry , histone , medicine , dna
Aim: Histone deacetylase (HDAC) is an attractive target for antitumor therapy. Therefore, the development of novel HDAC inhibitors is warranted. Materials & methods: A series of HDAC inhibitors based on N -hydroxycinnamamide fragment was designed as the clinically used belinostat analog using amide as the connecting unit. All target compounds were evaluated for their in vitro HDAC inhibitory activities and some selected compounds were tested for their antiproliferative activities. Conclusion: Among them, compound 7e showed an IC 50 value of 11.5 nM in inhibiting the HDAC in a pan-HDAC assay, being the most active compound of the series.