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:
Antiproliferative; Cancer; Phospholipase C; Thieno[2,3-b]pyridine; Tyrosyl-DNA phosphodiesterase I.
Copyright © 2016 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / pharmacology*
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Binding Sites
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Cell Line, Tumor
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Humans
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Hydrogen Bonding
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Molecular Docking Simulation
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Phospholipase C delta / antagonists & inhibitors
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Phospholipase C delta / chemistry
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Pyridines / chemical synthesis
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Pyridines / pharmacology*
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Quinolines / chemical synthesis
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Quinolines / pharmacology*
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Thiophenes / chemical synthesis
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Thiophenes / pharmacology*
Substances
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3-amino-2-((2'-chlorophenyl)carbamoyl)-5,6,7,8-tetrahydrothieno(2,3-b)quinolin-5-yl acetate
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Antineoplastic Agents
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Pyridines
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Quinolines
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Thiophenes
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PLCD1 protein, human
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Phospholipase C delta