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1,2-Benzisoxazole-3-acetamide derivatives as dual agents for DPP-IV inhibition and anticancer activity

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journal contribution
posted on 30.10.2018 by Shubhendu Karandikar, Rina Soni, Shubhangi S. Soman, Shweta Umar, Balakrishnan Suresh

Herein, we have designed various benzisoxazole acetamide derivatives with and without glycine spacer as DPP-IV inhibitors. Compounds 9a–d and 11a–e were synthesized and screened for their in vitro DPP-IV inhibition. Compounds 11a and 11c 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 9a–d and 11a–e for their anticancer activity using MTT assay against A549 and MCF7 cell lines. Compounds 9a–d without glycine spacer have shown good anticancer activity compared to compounds 11a–e with glycine spacer. Compound 9b has shown moderate activity with IC50 values 4.72 ± 0.72 and 4.39 ± 0.809 µM against A549 and MCF7 cell lines, respectively. Interestingly, compound 9c with cyano group has shown very good anticancer activity with IC50 2.36 ± 0.34 µM against MCF7 cell line as compared to fluorouracil with IC50 45.04 ± 1.02 µM.


One of the authors (RS) is thankful to Department of Science and Technology, Government of India for financial support vide reference no. SR/WOS-A/CS-1028/2014 under Women Scientist Scheme to carry out this work.