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Synthesis of novel derivatives of benzothiazole and benzothiazole isosters of expected activity against breast cancer

Mohamed A.Abdelgawad, Gehan M.Kamel

Combination of benzothiazole and benzothiazole isosteres (benzoxazole and benzimidazole) with certain anticancer active heterocyclic compounds, in one molecule, to increase its anticancer activity, was done and the study of this combination regarding the anticancer activity was made. In this study, substituted pyrazoles IIIa-c were prepared through diazotization of aminocompounds Ia-c followed by condensation with acetylacetone then hydrazinalysis of intermediates IIa-c (Scheme 1). Scheme 2 includes the reaction of the amino group of Ia-c with 2- chloromethyl-1H- benzimidazole (IV) to afford newcompoundsVa-c. The reaction of the amino group of Ia-c with pyrazolopyrimdine VIII gave the desired compounds IXa-c (Scheme 3). The cytotoxicity of compounds IIIa-c,Va-c and IXa-cwas evaluated against human breast carcinoma cell line (MCF7).