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Keywords:

  • antitumor agents;
  • medicinal chemistry;
  • natural products;
  • spirooxindoles;
  • total synthesis

Graphical Abstract

Thumbnail image of graphical abstract

1 % Inspiration, 99 % perspiration: Pyrrolidinyl-spirooxindole units are found in numerous bioactive natural products such as spirotryprostatin A (1). Synthetic advances toward the synthesis of this privileged structure have driven the development of analogue synthesis and programs of medicinal chemistry. The biological evaluation of analogues such as 2 shows great promise.

Abstract

The 3,3′-pyrrolidinyl-spirooxindole unit is a privileged heterocyclic motif that forms the core of a large family of alkaloid natural products with strong bioactivity profiles and interesting structural properties. Significant recent advances in the synthesis of this fused heterocyclic system have led to intense interest in the development of related compounds as potential medicinal agents or biological probes.