Author/Authors :
Mohammed M. Jaffar، نويسنده , , S. A. Everett، نويسنده , , M. A. Naylor، نويسنده , , S. G. Moore، نويسنده , , S. Ulhaq، نويسنده , , K. B. Patel، نويسنده , , M. R. L. Stratford، نويسنده , , J. Nolan، نويسنده , , P. Wardman، نويسنده , , I. J. Stratford، نويسنده ,
Abstract :
A series of regioisomeric derivatives of a 1-methylindole-4,7-dione were synthesised, substituted with a 2-acetoxybenzoate leaving group linked through the (indol-2-yl)methyl or (indol-3-yl)methyl (or propenyl) positions. Reductive elimination of the leaving group occurred from the (indol-3-yl)methyl derivatives but not the 2-substituted regioisomers, indicating that only the C-3 position may be utilised in bioreductively-activated drug delivery, which was demonstrated with an aspirin prodrug.
