Curcumin, a natural polyphenolic compound derived from turmeric (Curcuma longa L), has proven to exhibit biological activity towards different kinds of diseases. But the low oral bioavailability results in a limited application in clinic treatment. Recently, numerous curcumin derivatives were synthesized by the modification of three important functional groups: The aromatic o-methoxy phenolic group, a seven conjugated carbon linker and the β-diket one moiety. However, many people know curcumin only as an anticancer agent and overlook the diverse biological activities of curcumin and curcumin-based derivatives. In this article, we summarized the novel synthetic curcuminoids by different therapeutic activities including antioxidant activity, anti-HIV activity, stimulating activity of gastric emptying, anti-inflammatory activity, ACE inhibition activity, prevention of Parkinson's disease, anti-parasitism, anti-obesity, prevention of Alzheimer's disease, and antibacterial activity. The relation between structural features and activities were also investigated.