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In search of unprecedented tri and/or tetrapod pharmacophoric conjugates, a series of 32 new 4-ethyl-1<i>H</i>-benzo[<i>b</i>][1,4]diazepin-2(3<i>H</i>)-ones were synthesized and properly elucidated using MS, IR, NMR, and elemental analysis. <i>In vitro</i> investigation of 11 compounds of this series, using a panel of two human tumor cell lines namely; human breast adenocarcinoma (MCF-7), and human colorectal carcinoma (HCT-116), revealed promising cytotoxic activities. Among all synthesized compounds, analogue <b>9</b> displayed maximum cytotoxicity with IC₅₀ values of 16.19 ± 1.35 and 17.16 ± 1.54 μM against HCT-116 and MCF-7, respectively, compared to standard drug doxorubicin.