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Updated: Aug 14, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Furans, thiophenes and related heterocycles in drug discovery
Jeffrey B Sperry1, Dennis L Wright
1Dartmouth College, Department of Chemistry, Hanover, NH 03755, USA.
Abstract:
The five-membered aromatic heterocycles containing oxygen and sulfur are key building blocks used in medicinal chemistry applications. Furans, thiophenes and related azole analogs constitute an important class of compounds that are readily available, stable and easily functionalized. In this review, the authors survey the recent literature and highlight the application of such compounds in the development of therapeutic agents. This review focuses on two major strategies involving these compounds. The first is the use of these rings as intact scaffolds within the final target compound, and the second is the use of these compounds as convenient and flexible synthons for non-aromatic structural moieties.
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