Synthesis of 3′-azido-3′-deoxythymidine (AZT)—Cinchona alkaloid conjugates via click chemistry: Toward novel fluorescent markers and cytostatic agents

Bioorganic & Medicinal Chemistry Letters
2011.0

Abstract

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.

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