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Synthesis and antitumor activity of novel 2-(hetero)arylamino-benzothiazole derivatives

Despite advances in diagnosis and treatment cancer is still a second leading cause of death in the western world. Therefore, an area of major pharmaceutical interest over the last several decades has been development of small molecules with antitumor activity [1]. Two potential targets for drug design in cancer are DNA and different types of proteins like tyrosine kinases or topoisomerase I/II. So, the design of new intercalators, groove-binders and discovery of specific protein inhibitors are two important approaches in the search of new chemoterapeutic agents. A large number of benzothiazole derivatives show considerable biological activity [2]. 2-Amino-substituted benzothiazoles are reported as inhibitors of Src family kinases [3]. A significant number of tyrosine kinases are associated with cancers [4]. We prepared in multistep synthesis a series of new 2-amino substituted benzothiazoles from 4-aminobenzonitrile. All compounds were characterized by IR, 1H- and 13C-NMR spectroscopy and elemental analysis and tested on their antitumor activity.

Synthesis and antitumor activity; novel 2-(hetero)arylamino-benzothiazole derivatives

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