Selenium-containing small molecules have attracted considerable attention of
chemical and medicinal researchers owing to their various biological activities, such as
antitumor effects, cardiovascular protection, antibacterial or antiviral effects, immunoregulation
and nerve protection, among which the most promising area is antineoplasm.
In the past several decades, different kinds of organoselenium compounds, such as
selenides, seleno(iso)cyanates, substituted selenoureas, selenious esters and Se-containing
heterocycles have been reported as candidates of anti-cancer agents. Current reviews of
Se-containing anticancer compounds mainly concerned about the investigation of their
bioactivities, whereas, few attention has been addressed on their synthetic approaches.
Herein, we summarized methodologies recently developed to synthesize organoselenium
compounds with potent antineoplastic properties, which would be helpful for further design
and synthesis of new bioactive Se-containing molecules with diverse structural features.