Synthesis and antiproliferative activity of 2-chlorophenyl carboxamide thienopyridines

van Rensburg, Michelle; Leung, Euphemia; Haverkate, Natalie A.; Eurtivong, Chatchakorn; Pilkington, Lisa I.; Reynisson, Jóhannes; Barker, David

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.

Citation

van Rensburg, M., Leung, E., Haverkate, N. A., Eurtivong, C., Pilkington, L. I., Reynisson, J., & Barker, D. (2017). Synthesis and antiproliferative activity of 2-chlorophenyl carboxamide thienopyridines. Bioorganic and Medicinal Chemistry Letters, 27(2), 135-138. https://doi.org/10.1016/j.bmcl.2016.12.009

• Journal Article Type: Article
• Acceptance Date: Dec 2, 2016
• Online Publication Date: Dec 5, 2016
• Publication Date: 2017-01
• Deposit Date: Jun 13, 2023
• Journal: Bioorganic & Medicinal Chemistry Letters
• Print ISSN: 0960-894X
• Publisher: Elsevier
• Peer Reviewed: Peer Reviewed
• Volume: 27
• Issue: 2
• Pages: 135-138
• DOI: https://doi.org/10.1016/j.bmcl.2016.12.009
• Keywords: Organic Chemistry; Clinical Biochemistry; Drug Discovery; Pharmaceutical Science; Molecular Biology; Molecular Medicine; Biochemistry
• Additional Information: This article is maintained by: Elsevier; Article Title: Synthesis and antiproliferative activity of 2-chlorophenyl carboxamide thienopyridines; Journal Title: Bioorganic & Medicinal Chemistry Letters; CrossRef DOI link to publisher maintained version: https://doi.org/10.1016/j.bmcl.2016.12.009; Content Type: article; Copyright: © 2016 Elsevier Ltd. All rights reserved.