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Dichloroacetophenones targeting at pyruvate dehydrogenase kinase 1 with improved selectivity and antiproliferative activity: Synthesis and structure-activity relationships Journal article
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2018,Volume: 28,Issue: 21,Page: 3441-3445
Authors:  Zhang, Shao-Lin;  Yang, Zheng;  Hu, Xiaohui;  Tam, Kin Yip
Favorite | View/Download:17/0 | TC[WOS]:2 TC[Scopus]:0 | Submit date:2018/10/30
Pyruvate dehydrogenase kinase  Pyruvate dehydrogenase complex  Antiproliferative activity  Dichloroacetophenone  Kinase inhibition  
Identification of Novel Pyruvate Dehydrogenase Kinase 1 (PDK1) Inhibitors by Kinase Activity-Based High-Throughput Screening for Anticancer Therapeutics Journal article
ACS Combinatorial Science, 2018,Volume: 20,Issue: 11,Page: 660-671
Authors:  Zhang W.;  Hu X.;  Chakravarty H.;  Yang Z.;  Tam K.Y.
Favorite | View/Download:18/0 | TC[WOS]:0 TC[Scopus]:0 | Submit date:2018/12/18
cancer  high-throughput screening  pyruvate dehydrogenase kinase 1  small molecule inhibitors  Warburg effect  
Inhibition of pyruvate dehydrogenase kinase 1 enhances the anti-cancer effect of EGFR tyrosine kinase inhibitors in non-small cell lung cancer Journal article
EUROPEAN JOURNAL OF PHARMACOLOGY, 2018,Volume: 838,Page: 41-52
Authors:  Yang, Zheng;  Zhang, Shao-Lin;  Hu, Xiaohui;  Tam, Kin Yip
Favorite | View/Download:28/0 | TC[WOS]:3 TC[Scopus]:0 | Submit date:2018/10/30
Dichloroacetophenone  Epidermal Growth Factor Receptor  Tyrosine Kinase Inhibitor  Synergism  Hypoxia  Oxidative Phosphorylation  
Anticancer effects of some novel dichloroacetophenones through the inhibition of pyruvate dehydrogenase kinase 1 Journal article
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2018,Volume: 123,Page: 43-55
Authors:  Zhang, Shao-Lin;  Yang, Zheng;  Hu, Xiaohui;  Chakravarty, Harapriya;  Tam, Kin Yip
Favorite | View/Download:22/0 | TC[WOS]:4 TC[Scopus]:0 | Submit date:2018/10/30
Dichloroacetophenone  Pyruvate Dehydrogenase Kinase  Pyruvate Dehydrogenase Complex  Anticancer Activity  Metabolic Reprogramming  
Liquid Chromatography-Tandem Mass Spectrometry Method Revealed that Lung Cancer Cells Exhibited Distinct Metabolite Profiles upon the Treatment with Different Pyruvate Dehydrogenase Kinase Inhibitors Journal article
JOURNAL OF PROTEOME RESEARCH, 2018,Volume: 17,Issue: 9,Page: 3012-3021
Authors:  Zhang, Wen;  Hu, Xiaohui;  Zhou, Wei;  Tam, Kin Yip
Favorite | View/Download:21/0 | TC[WOS]:6 TC[Scopus]:0 | Submit date:2018/10/30
Aerobic Glycolysis  Azd7545  Dichloroacetate  Lc-ms/ms  Pyruvate Dehydrogenase Kinases  Cancer Metabolism  
Synthesis and biological evaluation of (R)-3,3,3-trifluoro-2-hydroxy-2methylpropionamides as pyruvate dehydrogenase kinase 1 (PDK1) inhibitors to reduce the growth of cancer cells Conference paper
Authors:  Zhang, Shao-Lin;  Zhang, Wen;  Yang, Zheng;  Hu, Xiaohui;  Tam, Kin Yip
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Pyruvate dehydrogenase kinase  Pyruvate dehydrogenase complex  Anti-proliferation  Binding affinity  
Phenyl butyrate inhibits pyruvate dehydrogenase kinase 1 and contributes to its anti-cancer effect Conference paper
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, Zhuhai, PEOPLES R CHINA, 2016-8-23-26
Authors:  Zhang, Wen;  Zhang, Shao-Lin;  Hu, Xiaohui;  Tam, Kin Yip
Favorite | View/Download:15/0 | TC[WOS]:6 TC[Scopus]:0 | Submit date:2018/10/30
Phenyl Butyrate  Cancer  Pyruvate Dehydrogenase  Pyruvate Dehydrogenase Kinase 1  Tumor Metabolism  
Synthesis and biological evaluation of (R)-3,3,3-trifluoro-2-hydroxy-2-methylpropionamides as pyruvate dehydrogenase kinase 1 (PDK1) inhibitors to reduce the growth of cancer cells Journal article
European Journal of Pharmaceutical Sciences, 2017,Volume: 110,Page: 87-92
Authors:  Zhang S.-L.;  Zhang W.;  Yang Z.;  Hu X.;  Tam K.Y.
Favorite | View/Download:12/0 | TC[WOS]:3 TC[Scopus]:0 | Submit date:2018/12/18
Anti-proliferation  Binding affinity  Pyruvate dehydrogenase complex  Pyruvate dehydrogenase kinase  
Unexpected Discovery of Dichloroacetate Derived Adenosine Triphosphate Competitors Targeting Pyruvate Dehydrogenase Kinase to Inhibit Cancer Proliferation Journal article
Journal of Medicinal Chemistry, 2016,Volume: 59,Issue: 7,Page: 3562-3568
Authors:  Zhang S.-L.;  Hu X.;  Zhang W.;  Tam K.Y.
Favorite | View/Download:2/0 | TC[WOS]:26 TC[Scopus]:0 | Submit date:2018/12/18
Development of dichloroacetamide pyrimidines as pyruvate dehydrogenase kinase inhibitors to reduce cancer cell growth: Synthesis and biological evaluation Journal article
RSC Advances, 2016,Volume: 6,Issue: 82,Page: 78762-78767
Authors:  Zhang S.-L.;  Zhang W.;  Xiao Q.;  Yang Z.;  Hu X.;  Wei Z.;  Tam K.Y.
Favorite | View/Download:7/0 | TC[WOS]:4 TC[Scopus]:0 | Submit date:2018/12/18