Literature DB >> 20189382

Inhibition of eEF2-K by thieno[2,3-b]pyridine analogues.

Jeffrey W Lockman1, Matthew D Reeder, Kazuyuki Suzuki, Kirill Ostanin, Ryan Hoff, Leena Bhoite, Harry Austin, Vijay Baichwal, J Adam Willardsen.   

Abstract

Several series of thieno[2-3-b]pyridine analogues were synthesized and screened for inhibitory activity against eukaryotic elongation factor-2 kinase (eEF2-K). Modifications around several regions of the lead molecules were made, with a ring fusion adjacent to the nitrogen on the thienopyridine core being critical for activity. The most active compound 34 shows an IC(50) of 170 nM against eEF2-K in vitro. 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20189382     DOI： 10.1016/j.bmcl.2010.02.005

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  9 in total

1.  Investigating the kinetic mechanism of inhibition of elongation factor 2 kinase by NH125: evidence of a common in vitro artifact.

Authors:  Ashwini K Devkota; Clint D J Tavares; Mangalika Warthaka; Olga Abramczyk; Kyle D Marshall; Tamer S Kaoud; Kivanc Gorgulu; Bulent Ozpolat; Kevin N Dalby
Journal:  Biochemistry       Date:  2012-03-05       Impact factor: 3.162

2.  Discovery of New Inhibitors of eEF2K from Traditional Chinese Medicine Based on In Silico Screening and In Vitro Experimental Validation.

Authors:  Qinghua Fu; Xiaomei Liu; Yan Li; Peng Wang; Tian Wu; Haihan Xiao; Yameng Zhao; Qichao Liao; Ziyi Song
Journal:  Molecules       Date:  2022-07-30       Impact factor: 4.927

Review 3.  Eukaryotic elongation factor 2 kinase as a drug target in cancer, and in cardiovascular and neurodegenerative diseases.

Authors:  Rui Liu; Christopher G Proud
Journal:  Acta Pharmacol Sin       Date:  2016-01-25       Impact factor: 6.150

4.  Using docking and alchemical free energy approach to determine the binding mechanism of eEF2K inhibitors and prioritizing the compound synthesis.

Authors:  Qiantao Wang; Ramakrishna Edupuganti; Clint D J Tavares; Kevin N Dalby; Pengyu Ren
Journal:  Front Mol Biosci       Date:  2015-03-19

5.  A high-throughput screening assay for eukaryotic elongation factor 2 kinase inhibitors.

Authors:  Ting Xiao; Rui Liu; Christopher G Proud; Ming-Wei Wang
Journal:  Acta Pharm Sin B       Date:  2016-05-21       Impact factor: 11.413

Review 6.  Progress in the Development of Eukaryotic Elongation Factor 2 Kinase (eEF2K) Natural Product and Synthetic Small Molecule Inhibitors for Cancer Chemotherapy.

Authors:  Bin Zhang; Jiamei Zou; Qiting Zhang; Ze Wang; Ning Wang; Shan He; Yufen Zhao; C Benjamin Naman
Journal:  Int J Mol Sci       Date:  2021-02-27       Impact factor: 5.923

Review 7.  Eukaryotic elongation factor-2 kinase (eEF2K) signaling in tumor and microenvironment as a novel molecular target.

Authors:  Didem Karakas; Bulent Ozpolat
Journal:  J Mol Med (Berl)       Date:  2020-05-07       Impact factor: 4.599

8.  Discovery of Novel eEF2K Inhibitors Using HTS Fingerprint Generated from Predicted Profiling of Compound-Protein Interactions.

Authors:  Atsushi Yoshimori; Enzo Kawasaki; Ryuta Murakami; Chisato Kanai
Journal:  Medicines (Basel)       Date:  2021-05-20

9.  Thieno[2,3-b]Pyridine Derivative Targets Epithelial, Mesenchymal and Hybrid CD15s+ Breast Cancer Cells.

Authors:  Sandra Marijan; Angela Mastelić; Anita Markotić; Nikolina Režić-Mužinić; Nikolina Vučenović; David Barker; Lisa I Pilkington; Jóhannes Reynisson; Vedrana Čikeš Čulić
Journal:  Medicines (Basel)       Date:  2021-06-22
  9 in total

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