Synthesis and antiproliferative activity of 2-chlorophenyl carboxamide thienopyridines

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• 作者：Michelle van Rensburg^a ; Euphemia Leung^b ; Natalie A. Haverkate^a ; Chatchakorn Eurtivong^a ; Lisa I. Pilkington^a ; Jó ; hannes Reynisson^a ; David Barker^a ; ^{d.barker@auckland.ac.nz}
• 关键词：Cancer ; Thieno[2 ; 3-b]pyridine ; Phospholipase C ; Tyrosyl-DNA phosphodiesterase I ; Antiproliferative
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2017
• 出版时间：15 January 2017
• 年：2017
• 卷：27
• 期：2
• 页码：135-138
• 全文大小：1032 K
• 卷排序：27

文摘

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.