Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening

2020 ◽  
Vol 192 ◽  
pp. 112189 ◽  
Author(s):  
Jian Liu ◽  
Jingxian Zhou ◽  
Fengjun He ◽  
Liang Gao ◽  
Yu Wen ◽  
...  
Keyword(s):  
Virtual Screening ◽  
Hdac Inhibitors ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

Design, synthesis and biological evaluation of β-boswellic acid based HDAC inhibitors as inducers of cancer cell death

2014 ◽  
Vol 24 (19) ◽  
pp. 4729-4734 ◽  
Author(s):  
Simmi Sharma ◽  
Mudassier Ahmad ◽  
Javeed Ahmad Bhat ◽  
Arvind Kumar ◽  
Manjeet Kumar ◽  
...  
Keyword(s):  
Cell Death ◽  
Cancer Cell ◽  
Hdac Inhibitors ◽  
Biological Evaluation ◽  
Boswellic Acid ◽  
Design Synthesis ◽  
Cancer Cell Death ◽  
Synthesis And Biological Evaluation

Structure and property based design, synthesis and biological evaluation of γ-lactam based HDAC inhibitors

2011 ◽  
Vol 21 (4) ◽  
pp. 1218-1221 ◽  
Author(s):  
Eunhyun Choi ◽  
Chulho Lee ◽  
Jung Eun Park ◽  
Jeong Jea Seo ◽  
Misun Cho ◽  
...  
Keyword(s):  
Hdac Inhibitors ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Structure And Property ◽  
Synthesis And Biological Evaluation

scholarly journals Design, synthesis and biological evaluation of β-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity

MedChemComm ◽  
2019 ◽  
Vol 10 (7) ◽  
pp. 1109-1115 ◽  
Author(s):  
Nina Reßing ◽  
Viktoria Marquardt ◽  
Christoph G. W. Gertzen ◽  
Andrea Schöler ◽  
Alexander Schramm ◽  
...  
Keyword(s):  
Hdac Inhibitors ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

Novel β-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity were synthesized.

scholarly journals Design, Synthesis, and Biological Evaluation of Dual c-Met/HDAC Inhibitors Bearing 2-Aminopyrimidine Scaffold

2020 ◽  
Vol 02 (03) ◽  
pp. e143-e149
Author(s):  
Qingwei Zhang ◽  
Guili Xu ◽  
Ya Bao ◽  
Minru Jiao ◽  
Jianqi Li
Keyword(s):  
Histone Deacetylase ◽  
Cell Lines ◽  
Hdac Inhibitors ◽  
Biological Evaluation ◽  
Antitumor Drugs ◽  
Design Synthesis ◽  
Ic50 Values ◽  
Hct 116 ◽  
Synthesis And Biological Evaluation ◽  
Antiproliferative Activities

AbstractA series of c-Met/histone deacetylase (HDAC) bifunctional inhibitors was designed and synthesized by merging pharmacophores of c-Met and HDAC inhibitors. Among them, the most potent compound, 2o, inhibited c-Met kinase and HDACs, with IC50 values of 9.0 and 31.6 nM, respectively, and showed efficient antiproliferative activities against both A549 and HCT-116 cancer cell lines with greater potency than an equimolar mixture of the respective inhibitors of the two enzymes: crizotinib and vorinostat (SAHA). Our study provided an efficient strategy for the discovery of multitargeted antitumor drugs.

Design, synthesis and biological evaluation of 1,4-benzodiazepine-2,5-dione-based HDAC inhibitors

2007 ◽  
Vol 17 (17) ◽  
pp. 4819-4823 ◽  
Author(s):  
Lynda Loudni ◽  
Joëlle Roche ◽  
Vincent Potiron ◽  
Jonathan Clarhaut ◽  
Christian Bachmann ◽  
...  
Keyword(s):  
Hdac Inhibitors ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

scholarly journals Design, synthesis and biological evaluation of small molecule inhibitors of CD4-gp120 binding based on virtual screening

2011 ◽  
Vol 19 (1) ◽  
pp. 91-101 ◽  
Author(s):  
Judith M. LaLonde ◽  
Mark A. Elban ◽  
Joel R. Courter ◽  
Akihiro Sugawara ◽  
Takahiro Soeta ◽  
...  
Keyword(s):  
Virtual Screening ◽  
Small Molecule ◽  
Small Molecule Inhibitors ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Gp120 Binding ◽  
Synthesis And Biological Evaluation
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