Synthesis and biological activity of neopeltolide and analogs

Abstract

Neopeltolide, a macrolide natural product of marine origin, was initially isolated from a deep-sea sponge belonging to the Neopeltidae family. This compound has garnered significant attention due to its intriguing structural complexity and remarkable biological potency. Since its discovery, the scientific community has reported over twenty distinct total syntheses, formal syntheses, and fragment syntheses of this natural product, along with developing more than eighty neopeltolide analogues with their corresponding biological evaluations. This comprehensive review systematically examines the biological profile of neopeltolide and elucidates its structure–activity relationships. We provide a detailed overview of the synthetic approaches and biological evaluations of neopeltolide and its structural analogs, with particular emphasis on the synthetic efforts that have contributed to understanding its structure–activity relationship.