A highly enantioselective intramolecular 1,3-dipolar cycloaddition yields novel pseudo-natural product inhibitors of the Hedgehog signalling pathway

Abstract

De novo combination of natural product (NP) fragments by means of efficient, complexity- and stereogenic character-generating transformations to yield pseudo-natural products (PNPs) may explore novel biologically relevant chemical space. Pyrrolidine-...

Synthesis of Complex Tetracyclic Fused Scaffolds Enabled by (3 + 2) Cycloaddition

“…In this regard, it often draws inspiration from the biological relevance and chemical diversity of natural products . The need to explore new chemical space has been facilitated by strategies such as fragment-based compound design. − For example, formal fragmentation of natural products and subsequent recombination, in various arrangements, can deliver novel analogues. − Such analogues, per se inaccessible through biosynthetic pathways, may inherit the biological and chemical properties of the original natural products and, thus, are called pseudo-natural products, a principle introduced by Waldmann et al that has been shown effective for identifying new biologically active compounds. − …”

“… 5 − 7 Such analogues, per se inaccessible through biosynthetic pathways, may inherit the biological and chemical properties of the original natural products and, thus, are called pseudo-natural products, a principle introduced by Waldmann et al that has been shown effective for identifying new biologically active compounds. 8 − 11 …”