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Synthesis and antiproliferative activity of 2-chlorophenyl carboxamide thienopyridines
Authors:Michelle van Rensburg  Euphemia Leung  Natalie A. Haverkate  Chatchakorn Eurtivong  Lisa I. Pilkington  Jóhannes Reynisson  David Barker
Affiliation:1. School of Chemical Sciences, University of Auckland, New Zealand;2. Auckland Cancer Society Research Centre and Department of Molecular Medicine and Pathology, University of Auckland, New Zealand
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.
Keywords:Cancer  Phospholipase C  Tyrosyl-DNA phosphodiesterase I  Antiproliferative
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