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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
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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.
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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
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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
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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
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aerobic glycolysis  AZD7545  dichloroacetate  LC-MS/MS  pyruvate dehydrogenase kinases  cancer 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.
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Anti-proliferation  Binding affinity  Pyruvate dehydrogenase complex  Pyruvate dehydrogenase kinase  
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
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Phenyl Butyrate  Cancer  Pyruvate Dehydrogenase  Pyruvate Dehydrogenase Kinase 1  Tumor Metabolism  
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.
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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.
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