Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors

2019 ◽  
Vol 173 ◽  
pp. 185-202 ◽  
Author(s):  
Chunhui Cheng ◽  
Fan Yun ◽  
Jie He ◽  
Sadeeq Ullah ◽  
Qipeng Yuan
Keyword(s):  
Histone Deacetylase ◽  
Hdac Inhibitors ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

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.

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

2020 ◽  
Vol 02 (02) ◽  
pp. e117-e123
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.

scholarly journals Design, synthesis, and biological evaluation of AV6 derivatives as novel dual reactivators of latent HIV-1

RSC Advances ◽  
2018 ◽  
Vol 8 (31) ◽  
pp. 17279-17292 ◽  
Author(s):  
Mingtao Ao ◽  
Zhenrui Pan ◽  
Yuqing Qian ◽  
Bowen Tang ◽  
Zeming Feng ◽  
...  
Keyword(s):  
Histone Deacetylase ◽  
Hdac Inhibitors ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Latent Hiv ◽  
Synthesis And Biological Evaluation ◽  
Hiv 1

As dual-acting HIV LRAs, compounds 12c and 12d could activate latent HIV-1 via the NFAT-required mechanism and as histone deacetylase (HDAC) inhibitors.

scholarly journals Novel 4-Oxoquinazoline-Based N-Hydroxypropenamides as Histone Deacetylase Inhibitors: Design, Synthesis, and Biological Evaluation

ACS Omega ◽  
2021 ◽  
Vol 6 (7) ◽  
pp. 4907-4920
Author(s):  
Duong T. Anh ◽  
Pham-The Hai ◽  
Le D. Huy ◽  
Hoang B. Ngoc ◽  
Trinh T. M. Ngoc ◽  
...  
Keyword(s):  
Histone Deacetylase ◽  
Histone Deacetylase Inhibitors ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation
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