875318-46-0Relevant articles and documents
Design, Synthesis, and Structure-Activity relationships of Evodiamine-Based topoisomerase (Top)/Histone deacetylase (HDAC) dual inhibitors
Dong, Guoqiang,Liang, Huixin,Liu, Dan,Meng, Xiangguo,Sheng, Chunquan,Wu, Shanchao,Zhu, Fugui
supporting information, (2022/03/16)
On the basis of synergistic effect between topoisomerase (Top) and histone deacetylase (HDAC) inhibitors, a series of novel evodiamine-based Top/HDAC dual inhibitors were designed and synthesized. Systematic structure?activity relationship (SAR) studies led to the discovery of compounds 29b and 45b, which simultaneously inhibited Top and HDAC and exhibited potent antitumor activities against the HCT116 cell line. Compounds 29b and 45b efficiently induced apoptosis with G2 cell cycle arrest and significantly inhibited cellular HDACs in HCT116 cells with good in vitro metabolic stabilities. Collectively, this work provides valuable SAR information and lead compounds for evodiamine-based Top/HDAC dual inhibitors.
CDK INHIBITORS CONTAINING A ZINC BINDING MOIETY
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, (2009/04/25)
The present invention relates to CDK inhibitors and their use in the treatment of cell proliferative diseases such as cancer. The compounds of the invention may further act as HDAC inhibitors.
AMINOPHENYL DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE
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Page/Page column 26, (2008/06/13)
This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X and Y have defined meanings, having histone deacet
