Quantum dots (QDs) are nanoparticles or nanocrystals of a semiconducting material with diameters in the range of 2-10 nm and fluorescent semiconductor QDs have attracted lot of scientific attention over the last decade for their use in biomedical applications, whereas their potential toxicity and instability in biological environment has puzzled clinical researchers. Their surface modification and functionalization have been subjected for significant progress over last several years to make them versatile probes for biomedical applications, especially in biological imaging. This practice is facilitated with biological molecules with broad absorption spectra, bright emission, and physical and photophysical robustness along with current state of the art of the synthesis, modification, and bioconjugation of prepared QDs. These surface-modified QDs could be further used for brain-targeted imaging for getting precise localization of tumor tissues within normal brain parenchyma to achieve accurate diagnostic biopsy and complete surgical resection for improved surgical management of brain tumors as potent optical imaging and optical spectroscopy tools.