Abstract: Curcumin is the main active ingredient of Curcuma longa, which has been reported to possess many pharmacological activities, such as anti-tumor, anti-inflammatory and anti-oxidation. Unfortunately, curcumin has a weak pharmacokinetic profile in vivo, which significantly inhibits its clinical application. In recent years, with curcumin as the lead compound, a large number of monocarbonyl curcumin analogues have been synthesized, and the pharmacological activities were evaluated. This article briefly outlines the synthetic method, activity test and structure-activity relationship of three kinds of curcumin analogues from the perspective of spacers, respectively. At last, the design and synthesis of novel curcumin analogues are prospected, which was expected to develop many efficient curcumin analogues.