1,2-Benzisoxazole-3-acetamide derivatives as dual agents for DPP-IV inhibition and anticancer activity KarandikarShubhendu SoniRina SomanShubhangi S. UmarShweta SureshBalakrishnan 2018 <p>Herein, we have designed various benzisoxazole acetamide derivatives with and without glycine spacer as DPP-IV inhibitors. Compounds <b>9a–d</b> and <b>11a–e</b> were synthesized and screened for their <i>in vitro</i> DPP-IV inhibition. Compounds <b>11a</b> and <b>11c</b> showed moderate activity for DPP-IV inhibition, whereas other remained inactive at 25–200 µM concentrations. DPP-IV inhibition can be a good strategy for modulating diabetes and cancer; hence, we have screened compounds <b>9a–d</b> and <b>11a–e</b> for their anticancer activity using MTT assay against A549 and MCF7 cell lines. Compounds <b>9a–d</b> without glycine spacer have shown good anticancer activity compared to compounds <b>11a–e</b> with glycine spacer. Compound <b>9b</b> has shown moderate activity with IC<sub>50</sub> values 4.72 ± 0.72 and 4.39 ± 0.809 µM against A549 and MCF7 cell lines, respectively. Interestingly, compound <b>9c</b> with cyano group has shown very good anticancer activity with IC<sub>50</sub> 2.36 ± 0.34 µM against MCF7 cell line as compared to fluorouracil with IC<sub>50</sub> 45.04 ± 1.02 µM.</p> <p></p>