This article described a small molecule that can specifically bind to leukemia stem cells (LSC), a special subgroup of leukemia cells that are resistant to chemotherapy, and can regenerate leukemia cells to cause leukemia recurrence. This small molecule can potentially target and kill LSC. A nanoparticle drug delivery system was also developed. These nanoparticles are loaded with chemotherapeutic drug inside, and decorated with the LSC-targeting molecule on the surface. The resulting nanoparticles can work like “smart missiles” to seek and kill LSC after intravenous injection.