2-Substituted Benzothiazoles as Antiproliferative Agents: Novel Insights on Structure-Activity Relationships

Given the wide spectrum of biological activities, benzothiazoles represent privileged scaffolds in medicinal chemistry, useful in drug discovery programs to modulate biological activities of lead compounds. A large body of knowledge about benzothiazoles has been reported in scientific literature, describing their antimicrobial, anticonvulsant, neuroprotective, anti-inflammatory, and antiproliferative effects. This review summarizes the results obtained in the structure-activity relationship studies on antiproliferative benzothiazoles, focusing on 2-substituted derivatives and on mechanism of actions responsible for the antitumor effects of this class of compounds.