CAS 247564-66-5: 4,6-Difluoroindole-2-carboxylic acid

4,6-Difluoroindole-2-carboxylic acid (4,6-DFI) is a compound that inhibits tumour growth and has significant antitumour activity. This drug has been shown to bind to the active site of protein kinase A (PKA) and inhibit its function. 4,6-DFI also inhibits the proliferation of cancer cells in vitro by inducing apoptosis. The inhibitory effects on PKA are due to its structural similarity with bioisosteres of the natural substrate ATP. 4,6-DFI is synthesised from 3,5-dichloroindole through a series of chemical reactions including condensation with malonic acid chloride followed by diazotisation and coupling with 2-(4,6-difluorophenyl)-1,3-propanediol. This process requires a number of steps under acidic conditions and thus is not suitable for large scale production.

4,6-Difluoroindole-2-carboxylic acid