In this work, a simple, low-cost and one-step microwave approach has been demonstrated for the synthesis of water-soluble carbon dots (C-dots). The average size of the resulting C-dots is about 4 nm. From the photoluminescence (PL) measurements, the C-dots exhibit excellent biocompatibility and intense PL with the high quantum yield (QY) at Ca. 25%. Significantly, the C-dots have excellent biocompatibility and the capacity to specifically target the cells overexpressing the folate receptor (FR). These exciting results indicate the as-prepared C-dots are promising biocompatible probe for cancer diagnosis and treatment. (C) 2015 Elsevier Inc. All rights reserved.