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Bladder cancer is one of the deadly cancers with very limited options of treatment and lack of new drugs. Cisplatin, doxorubicin and thiotepa are the drugs mostly used in therapy. Nine new N-cycloheptyl-substituted- 2,3-dihydro-1,3- benzothiazole-2-carboxamide derivatives were designed using structure based drug discovery. The designed compounds were docked to ascertain their binding against balder cancer cell lines (PDB code 3ERT). structure. The designed compounds were synthesised and characterized using different spectroscopic techniques. These novel compounds were evaluated on the MTT assay for there in vitro efficiency using the TCP1020 cell lines. The compounds 4e and 4i shown good inhibition. Two compounds of the series exhibit promising results which are in agreement with the in silico studies. The most potent compound against TCP1020 cell lines was compound 4i; IC50 = 7.8 μM. The activity of the 4i will be due to the inhibition of estrogenic binding receptor. [ABSTRACT FROM AUTHOR]