Cancer is one of the leading causes of death worldwide. Because each person’s cancer may be unique, diagnosing and treating cancer is challenging. Advances in nanomedicine have made it possible to detect tumors and quickly investigate tumor cells at a cellular level in contrast to prior diagnostic techniques. Quantum dots (QDs) are functional nanoparticles reported to be useful for diagnosis. QDs are semiconducting tiny nanocrystals, 2–10 nm in diameter, with exceptional and useful optoelectronic properties that can be tailored to sensitively report on their environment. This review highlights these exceptional semiconducting QDs and their properties and synthesis methods when used in cancer diagnostics. The conjugation of reporting or binding molecules to the QD surface is discussed. This review summarizes the most recent advances in using QDs for in vitro imaging, in vivo imaging, and targeted drug delivery platforms in cancer applications.