Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 21, Issue 2, Pages 723-726Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.11.127
Keywords
Nucleosides; AZT; Cinchona alkaloids; Click chemistry; Conjugation
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Funding
- Ministry of Science and Higher Education [N N204 343037]
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Novel nucleoside-Cinchona alkaloid conjugates were synthesized using 'click' chemistry approach based on the copper(I) catalyzed Huisgen azide-alkyne cycloaddition. Two series of conjugates were prepared employing 3'-azido-3'-deoxythymidine (AZT) as the azide component and the four 10,11-didehydro Cinchona alkaloids as well as their 9-O-propargyl ethers as the alkyne components. All obtained conjugates showed strong fluorescence emission and some of them exhibited marked cytotoxic activity in vitro. (C) 2010 Elsevier Ltd. All rights reserved.
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