Synthesis of benzothiazole derivatives and their biological evaluation as anticancer agents

This article describes the synthesis and the biological evaluation of two sets of benzothiazole derivatives bearing at C-2 an arylamide (1a–e, 2a–e) or an arylurea (3a–d, 4a–d) moiety. Five compounds (3d and 4a–d) were selected and screened by the National Cancer Institute for the in vitro primary anticancer assay against a panel of 60 human tumor cell lines. Compounds 4a and 4c showed interesting anticancer activities, more marked for compound 4c. All compounds were also submitted to a preliminary in vitro assay as potential inhibitors of the ubiquitin-activating enzyme (E1), but they lacked significant activity.