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  • Title: Synthesis of combinatorial libraries of 3,4,5-trisubstituted 2(5H)-furanones. Part One: Construction of a sub-library of halogenated 5-alkoxy-2(5H)-furanones.
    Author: Lattmann E, Billington DC, Langley CA.
    Journal: Drug Des Discov; 1999 Nov; 16(3):237-42. PubMed ID: 10624569.
    Abstract:
    Starting from furfural, 5-hydroxy-3,4-dihalo-2(5H)-furanones and 5-hydroxy-4 chloro-2(5H)-furanone were converted into 3 sublibraries of halogenated 5-alkoxy-2(5H)-furanones. The reactivity of 24 halogenated 5-alkoxy2(5H)-furanones was chemically evaluated by using 4 selected amines for subsequent reactions. The biological evaluation of the pseudo-muco halogen esters resulted in the discovery of a lead structure with potent anti-cancer activity.
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