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.
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.
Lattmann
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E
Pharmaceutical Sciences Research Institute, Aston University, Birmingham, England. e.lattmann@aston.ac.uk
Billington
D C
DC
Langley
C A
CA
D020650:Combinatorial Chemistry Techniques; D015195:Drug Design; D005663:Furans / Q000138:chemical synthesis* / Q000737:chemistry; D006219:Halogens / Q000737:chemistry*
D005663:Furans; D006219:Halogens