The synthesis of water-soluble and low-cytotoxicity quantum dots (QDs) in aqueous solution has received much attention recently. A one-step and convenient method has been developed for synthesis of water-soluble glutathione (GSH)-capped and Zn(2+)-doped CdTe QDs via a refluxing route. Because of the addition of Zn ions and the epitaxial growth of a CdS layer, the prepared QDs exhibit superior properties, including strong fluorescence, minimal cytotoxicity, and enhanced biocompatibility. The optical properties of QDs are characterized by UV-vis and fluorescence (FL) spectra. The structure of QDs was verified by transmission electron microscopy (TEM), X-ray diffraction (XRD), X-ray photoelectron spectrometry (XPS), energy dispersive spectroscopy (EDS), atomic absorption spectrometry (AAS), and Fourier transform infrared spectroscopy (FTIR). Furthermore, the low cytotoxicity of the prepared QDs was proved by the microcalorimetric technique and inductively coupled plasma-atomic emission spectrometry (ICP-AES).