2016-2015
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Diversity-oriented one-pot multicomponent synthesis of spirooxindole derivatives and their biological evaluation for anticancer activities(Tetrahedron 2016, 72, 8523-8536)

Graphic Abstract

  

ABTRACT

Desicribed herein is afacile and efficient methodologyfordiversity-oriented one-pot multicomponent synthesis of 3-aminomethyl quaternary carbon oxindole fused five-membered carbocyclic spirooxindoles5viaknoevenagel condensation/Michael/cyclization and then aminomethylation reaction.A wide variety ofproductswith varying degrees of substitution around it,were obtained smoothlywith high efficiency (up to overall yield 73% and >20:1 diastereoselectivity).In particular, their biological activitiesagainst these three cell linesK562,A549 and PC-3have been evaluated.These results suggestedthatmost of3-aminomethyl quaternary carbon oxindole fused five-membered carbocyclic spirooxindoles5 showed equipotent or more potent than the positive control of Cisplatin (up to 3.4 times).