4.5 Article

Solvent effect on copper-catalyzed azide-alkyne cycloaddition (CuAAC): Synthesis of novel triazolyl substituted quinolines as potential anticancer agents

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 22, Issue 10, Pages 3455-3459

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.03.091

Keywords

Click chemistry; Azide; Alkyne; Quinoline; Cancer

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A regioselective route to novel mono triazolyl substituted quinolines has been developed via copper-catalyzed azide-alkyne cycloaddition (CuAAC) of 2,4-diazidoquinoline with terminal alkynes in DMF. The reaction provided bis triazolyl substituted quinolines when performed in water in the presence of Et3N. A number of the compounds synthesized showed promising anti-proliferative properties when tested in vitro especially against breast cancer cells. (C) 2012 Elsevier Ltd. All rights reserved.

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