2-Aminobenzothiazole: A Privileged Scaffold for Tyrosine Kinase–Targeted Anticancer Agents

2-Aminobenzothiazole’s planar structure and tendency to bind to a diverse set of oncogenic targets have made 2-aminobenzothiazole a highly sought heterocyclic in research for anticancer agents. In the past 10 years, intense research in medicinal chemistry has clarified that carefully planned substitution for benzothiazole can yield highly efficient and specific anticancer agents. In this critical assessment, we will specifically evaluate both research and efforts related to 2-aminobenzothiazole-based anticancer agents between 2015 and 2024 for their anticancer targets, SAR relationship, and mechanism of action. In particular, we highlight 2-aminobenzothiazole-based compounds targeting CDKs, Aurora kinase, RAF kinase, and various receptor and non-receptor tyrosine kinases such as EGFR, VEGFR-2, CSF1R, MET, FAK, and DYRK2. Besides inhibition of kinase activity, other non-kinase targets are systematically analysed and introduced in this patent review. These include BCL-2 family members, HDACs, epigenetic modifiers (LSD1, NSD1, FTO), HSP90, mutant p53, and DNA topoisomerases. Substitutions at the C-2, C-5, C-6, and C-7 positions of the benzothiazole ring are examined thoroughly about t