Screening small molecules having anti-aging effect and researching the mechanism are of great practical significance for discovering new effective targets for treatment of age-related diseases and tumors, developing new drugs and promoting human health. What is more important is that these small molecules can be used as breakthrough points for the specific molecular mechanisms of aging, cancer and other biological phenomena via in-depth study. And this has an important role in promoting the development of molecular biology and other related life sciences. This article summarizes some representative anti-aging small molecules of the past decade or two and focuses on their molecular mechanisms.