Prostate cancer possesses the highest occurrence rate and is the second-paramount disease that causes canceraffiliated
death among men in the United States. Approximately 30,000 men die each year of castration-resistant prostate
cancer due to the inevitable progression of resistance to first-line treatment with docetaxel. The safety profile of dietary
curcumin in humans has been well-documented, and its therapeutic prospect in treating prostate cancer, especially for
castration-resistant prostate cancer, has been evidenced in several cell culture systems and human xenograft mouse models.
The critical disadvantage of curcumin as a drug candidate is its low bioavailability caused by poor water solubility and rapid in vivo
metabolism. Curcumin is characteristic of regulating multiple targets, representing a good example for the philosophy to search for multitargeted
drugs in the realm of drug design and drug development. This feature, together with its potential in treating castration-resistant
prostate cancer and its safety profile, enables curcumin to serve as an ideal lead compound for the design and syntheses of curcuminbased
agents with improved potential for the clinical therapies of prostate cancer. Several researches aiming to improve its bioavailability
and potency resulted in the discovery and development of a wealth of curcumin-based compounds with an enhanced anticancer potential
and/or an improved pharmacokinetic profile. This review starts with a brief summarization of the prospect of curcumin in treating
prostate cancer and its mechanisms of action, then provides an in-depth overview of current development of curcumin-based anti-prostate
cancer agents and their structure-activity relationships, and ends with the syntheses and pharmacokinetic studies of curcumin.