A newly designed benzothiazolo-quinazolone series was synthesized by an aromatic amine and potassium thiocyanate in the presence of bromine in glacial acetic acid, and the final product was obtained by subsequent reaction with 5-arylamido/imidoalkyl-2-chlorobenzoic acid in the presence of potassium carbonate and further cyclization with sulphuric acid. A preliminary radiolabelling study with technetium shows a promising potential for further in vivo evaluation. Anti-bacterial, anti-viral and anti-tumor activities were evaluated for biological properties. Lead compounds are able to block epidermal growth factor receptor (EGFR) in human breast adenocarcinoma cell line, MCF-7.

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