Literature DB >> 27979592

Synthesis and antiproliferative activity of 2-chlorophenyl carboxamide thienopyridines.

Michelle van Rensburg1, Euphemia Leung2, Natalie A Haverkate1, Chatchakorn Eurtivong1, Lisa I Pilkington1, Jóhannes Reynisson1, David Barker3.   

Abstract

3-Amino-2-arylcarboxamide-thieno[2,3-b]pyridines are a known class of antiproliferative compounds with activity against the phospholipase C enzyme. To further investigate the structure activity relationships of these derivatives a series of analogues were prepared modifying key functional groups. It was determined that modification of the 3-amino and 2-aryl carboxamide functionalities resulted in complete elimination of activity, whilst modification at C-5 allowed compounds of greater activity to be prepared.
Copyright © 2016 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Antiproliferative; Cancer; Phospholipase C; Thieno[2,3-b]pyridine; Tyrosyl-DNA phosphodiesterase I

Mesh:

Substances:

Year:  2016        PMID: 27979592     DOI: 10.1016/j.bmcl.2016.12.009

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


  6 in total

1.  Investigation into Improving the Aqueous Solubility of the Thieno[2,3-b]pyridine Anti-Proliferative Agents.

Authors:  Ayesha Zafar; Lisa I Pilkington; Natalie A Haverkate; Michelle van Rensburg; Euphemia Leung; Sisira Kumara; William A Denny; David Barker; Ali Alsuraifi; Clare Hoskins; Jóhannes Reynisson
Journal:  Molecules       Date:  2018-01-11       Impact factor: 4.411

2.  GPCR Modulation of Thieno[2,3-b]pyridine Anti-Proliferative Agents.

Authors:  Ayesha Zafar; Suat Sari; Euphemia Leung; Lisa I Pilkington; Michelle van Rensburg; David Barker; Jóhannes Reynisson
Journal:  Molecules       Date:  2017-12-18       Impact factor: 4.411

3.  Disruption of Crystal Packing in Thieno[2,3-b]pyridines Improves Anti-Proliferative Activity.

Authors:  Natalie A Haverkate; Euphemia Leung; Lisa I Pilkington; David Barker
Journal:  Molecules       Date:  2022-01-27       Impact factor: 4.411

4.  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

5.  Tethered Aryl Groups Increase the Activity of Anti-Proliferative Thieno[2,3-b]Pyridines by Targeting a Lipophilic Region in the Active Site of PI-PLC.

Authors:  Natalie A Haverkate; Euphemia Leung; Lisa I Pilkington; David Barker
Journal:  Pharmaceutics       Date:  2021-11-26       Impact factor: 6.321

6.  Validating TDP1 as an Inhibition Target for the Development of Chemosensitizers for Camptothecin-Based Chemotherapy Drugs.

Authors:  Euphemia Leung; Jinal Patel; Jennifer A Hollywood; Ayesha Zafar; Petr Tomek; David Barker; Lisa I Pilkington; Michelle van Rensburg; Ries J Langley; Nuala A Helsby; Christopher J Squire; Bruce C Baguley; William A Denny; Jóhannes Reynisson; Ivanhoe K H Leung
Journal:  Oncol Ther       Date:  2021-06-23
  6 in total

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