The design, synthesis and biological evaluation of novel thiamin diphosphate analog inhibitors against the pyruvate dehydrogenase multienzyme complex E1 from Escherichia coli

2014 ◽  
Vol 12 (44) ◽  
pp. 8911-8918 ◽  
Author(s):  
Lingling Feng ◽  
Junbo He ◽  
Haifeng He ◽  
Lulu Zhao ◽  
Lingfu Deng ◽  
...  
Keyword(s):  
Pyruvate Dehydrogenase ◽  
Potent Inhibitor ◽  
Binding Mode ◽  
Biological Evaluation ◽  
The Novel ◽  
Multienzyme Complex ◽  
Thiamin Diphosphate ◽  
Design Synthesis ◽  
E Coli ◽  
Synthesis And Biological Evaluation

Optimal binding mode for the novel potent inhibitor 4j against PDHc-E1 from E. coli.

Design, synthesis, biological evaluation and molecular docking of amide and sulfamide derivatives as Escherichia coli pyruvate dehydrogenase complex E1 inhibitors

RSC Advances ◽  
2016 ◽  
Vol 6 (6) ◽  
pp. 4310-4320 ◽  
Author(s):  
Haifeng He ◽  
Jiangtao Feng ◽  
Junbo He ◽  
Qin Xia ◽  
Yanliang Ren ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Molecular Docking ◽  
Pyruvate Dehydrogenase ◽  
Pyruvate Dehydrogenase Complex ◽  
Binding Mode ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
E Coli ◽  
Dehydrogenase Complex

Optimal binding mode of novel E. coli PDHc E1 inhibitor 9d.

Design, Synthesis and Biological Evaluation of the Novel Antitumor Agent Aurone Derivatives

2013 ◽  
Vol 781-784 ◽  
pp. 1235-1239
Author(s):  
Qian Nan Guo ◽  
Lei Lv ◽  
Yao Zhou ◽  
Peng Yu ◽  
Yuou Teng
Keyword(s):  
Biological Activities ◽  
Antitumor Agent ◽  
Biological Evaluation ◽  
The Novel ◽  
Pharmacological Activities ◽  
Design Synthesis ◽  
H Nmr ◽  
Wide Range ◽  
Inhibitory Activities ◽  
Synthesis And Biological Evaluation

Aurones belong to a class of heterocyclic flavonoids which contains a benzofuran element associated with a benzylidene linked in position 2. Aurones possess a wide range of pharmacological activities and biological activities, such as antitumor, antifungal, phytoalexin and so on. A novel series of 2-ayl-yl (5-methacrylate) aurone analogues were synthesized in six steps with the overall yield of 11%-13% and characterized by 1H NMR. Among the key intermediates and target compounds, 2-(2-furan-ylmethylene)-5-methacrylate-benzofuran-3(2H)-one (7a) and 2-(2-thienyl-ylmethylene)-5-methacrylate-benzofuran-3(2H)-one (7b) have never been reported before. Primary biological activities evaluation showed that 7a exhibited good inhibitory activities against K562 with an IC50 of 2.18 μM and against HepG2 with an IC50 of 3.95μM.

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