Pd-Catalyzed Coupling of Bromo-N-(β-glucopyranpsyl)quinolin-2-ones with Amides: Synthesis of N-glucosyl-6BrCaQ Conjugates with Potent Anticancer Activity

Abstract

A series of N-glycosyl- 6BrCaQ conjugates was synthesized through a Pd-catalyzed cross-coupling reaction between brominated N-glycosyl quinolin-2-one derivatives and various nitrogen nucleophiles. Antiproliferative assays revealed that this new series of analogues represents a promising class of antitumor compounds as illustrated by the high biological activity observed for several derivatives towards different cancer cell lines compared to the non-glycosylated congeners.

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Keywords

N-glycosides, HPS90, TRAP1, Buchwald-Hartwig Cross-Coupling, Antiproleferative activity

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