953434-83-8Relevant academic research and scientific papers
Design and Synthesis of Novel N-(2-aminophenyl)benzamide Derivatives as Histone Deacetylase Inhibitors and Their Antitumor Activity Study
La, Minh Thanh,Jeong, Byung-Hoon,Kim, Hee-Kwon
supporting information, p. 740 - 743 (2021/03/16)
Histone deacetylases (HDACs) are promising therapeutic targets for cancer therapy because inhibition of HDACs triggers growth arrest or apoptosis of tumor cells. In the present study, a new series of fluorinated N-(2-aminophenyl)benzamide derivatives were synthesized to investigate potential inhibition of HDACs and associated anticancer activity. Among the synthesized derivatives, compound 24a showed potent inhibitory activity of HDACs and higher antitumor efficacy in human cancer cell lines (HCT-116, MCF-7, and A549) compared with SAHA. Moreover, animal studies demonstrated that compound 24a showed potent in vivo antitumor efficacy in an HCT-116 colon cancer xenograft mouse model.
Design, synthesis and biological evaluation of colchicine derivatives as novel tubulin and histone deacetylase dual inhibitors
Zhang, Xuan,Kong, Yannan,Zhang, Jie,Su, Mingbo,Zhou, Yubo,Zang, Yi,Li, Jia,Chen, Yi,Fang, Yanfen,Zhang, Xiongwen,Lu, Wei
, p. 127 - 135 (2015/04/14)
A new class of colchicine derivatives were designed and synthesized as tubulin-HDAC dual inhibitors. Biological evaluations of these hybrids included the inhibitory activity of HDAC, tubulin polymerization analysis, in vitro cell cycle analysis in HCT-116 cells and cytotoxicity against different cancer cell lines. Hybrid 6d behaved as potent HDAC-tubulin dual inhibitor and showed comparable cytotoxicity with colchicine. Compound 11a exhibited powerful tubulin inhibitory activity, moderate anti-HDAC activity and the most potent cytotoxicity (IC50 Combining double low line 2-105 nM).
Image-guided synthesis reveals potent blood-brain barrier permeable histone deacetylase inhibitors
Seo, Young Jun,Kang, Yeona,Muench, Lisa,Reid, Alicia,Caesar, Shannon,Jean, Logan,Wagner, Florence,Holson, Edward,Haggarty, Stephen J.,Weiss, Philipp,King, Payton,Carter, Pauline,Volkow, Nora D.,Fowler, Joanna S.,Hooker, Jacob M.,Kim, Sung Won
, p. 588 - 596 (2014/08/05)
Recent studies have revealed that several histone deacetylase (HDAC) inhibitors, which are used to study/treat brain diseases, show low blood-brain barrier (BBB) penetration. In addition to low HDAC potency and selectivity observed, poor brain penetrance
SILICON DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS
-
Page/Page column 55, (2009/04/25)
The present invention relates to a novel class of Silicon derivatives. The Silicon compounds can be used to treat cancer. The Silicon compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation,
4-CARBOXYBENZYLAMINO DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS
-
Page/Page column 62, (2009/03/07)
The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selecti
PHOSPHORUS DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS
-
Page/Page column 160, (2008/06/13)
The present invention relates to a novel class of phosphorus derivatives. The phosphorus compounds can be used to treat cancer. The phosphorus compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differe
Optimization of biaryl Selective HDAC1&2 Inhibitors (SHI-1:2)
Witter, David J.,Harrington, Paul,Wilson, Kevin J.,Chenard, Melissa,Fleming, Judith C.,Haines, Brian,Kral, Astrid M.,Secrist, J. Paul,Miller, Thomas A.
, p. 726 - 731 (2008/12/23)
A class of biaryl benzamides was identified and optimized as selective HDAC1&2 inhibitors (SHI-1:2). These agents exhibit selectivity over class II HDACs 4-7, as well as class I HDACs 3 and 8; providing examples of selective HDAC inhibitors for the HDAC i
BENZAMIDE DERIVATIVES AS INHIBITORS OF HISTONE DEACETYLASE
-
Page/Page column 94, (2008/06/13)
The invention relates to the inhibition of histone deacetylase. The invention provides compounds which are derivatives of benzamide and suitable in methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions .
