1429129-72-5Relevant academic research and scientific papers
Targeting epigenetic reader and eraser: Rational design, synthesis and in vitro evaluation of dimethylisoxazoles derivatives as BRD4/HDAC dual inhibitors
Zhang, Zhimin,Hou, Shaohua,Chen, Hongli,Ran, Ting,Jiang, Fei,Bian, Yuanyuan,Zhang, Dewei,Zhi, Yanle,Wang, Lu,Zhang, Li,Li, Hongmei,Zhang, Yanmin,Tang, Weifang,Lu, Tao,Chen, Yadong
, p. 2931 - 2935 (2016)
The bromodomain protein module and histone deacetylase (HDAC), which recognize and remove acetylated lysine, respectively, have emerged as important epigenetic therapeutic targets in cancer treatments. Herein we presented a novel design approach for cancer drug development by combination of bromodomain and HDAC inhibitory activity in one molecule. The designed compounds were synthesized which showed inhibitory activity against bromodomain 4 and HDAC1. The representative dual bromodomain/HDAC inhibitors, compound 11 and 12, showed potent antiproliferative activities against human leukaemia cell line K562 and MV4-11 in cellular assays. This work may lay the foundation for developing dual bromodomain/HDAC inhibitors as potential anticancer therapeutics.
Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands
Hewings, David S.,Fedorov, Oleg,Filippakopoulos, Panagis,Martin, Sarah,Picaud, Sarah,Tumber, Anthony,Wells, Christopher,Olcina, Monica M.,Freeman, Katherine,Gill, Andrew,Ritchie, Alison J.,Sheppard, David W.,Russell, Angela J.,Hammond, Ester M.,Knapp, Stefan,Brennan, Paul E.,Conway, Stuart J.
, p. 3217 - 3227 (2013/06/04)
The bromodomain protein module, which binds to acetylated lysine, is emerging as an important epigenetic therapeutic target. We report the structure-guided optimization of 3,5-dimethylisoxazole derivatives to develop potent inhibitors of the BET (bromodom
