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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:23/0
|
TC[WOS]:
2
TC[Scopus]:
2
|
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:20/0
|
TC[WOS]:
0
TC[Scopus]:
2
|
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:36/0
|
TC[WOS]:
3
TC[Scopus]:
6
|
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:29/0
|
TC[WOS]:
4
TC[Scopus]:
5
|
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:30/0
|
TC[WOS]:
6
TC[Scopus]:
6
|
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
Favorite
|
View/Download:9/0
|
TC[WOS]:
3
TC[Scopus]:
3
|
Submit date:2018/10/30
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:17/0
|
TC[WOS]:
6
TC[Scopus]:
10
|
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:16/0
|
TC[WOS]:
3
TC[Scopus]:
3
|
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:3/0
|
TC[WOS]:
26
TC[Scopus]:
26
|
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:10/0
|
TC[WOS]:
4
TC[Scopus]:
4
|
Submit date:2018/12/18