Silver‐Catalyzed Tandem Reaction of β‐Alkynyl Ketones toward Spiro[isochromene‐1,4′‐quinoline] with Anticancer Activities.

Spirocyclic frameworks could enhance the drug‐like properties of planar bioactive molecules by increasing their three‐dimensionality, making the development of synthetic methodology and bioactivity assays for spiro compounds highly attractive. This work reported the silver‐catalyzed tandem cycloisomerization/Povarov reaction between β‐alkynyl ketones and hexahydro‐1,3,5‐triazines, access to spiro[isochromene‐1,4'‐quinoline]. This synthetic protocol was characterized by remarkable efficiency, low catalyst‐loading and high diastereoselectivity. Moreover, the spirocyclic quinolines exhibited good cytotoxicity in U937 cells by activating the Notch‐signaling pathway exclusively. [ABSTRACT FROM AUTHOR]