An efficient synthesis of spiro[indoline-3, 7′-pyrrolo[1, 2-c]imidazole] is achieved through a three-component reaction of isatins, malononitrile, and hydantoin/2-thiohydantoin in water catalysed by NaHCO3. All the target compounds were screened for the Cell Division Cycle 25 Phosphatase B (CDC25B) inhibitory activities.