Design, synthesis, and biological evaluation of phenyl-isoxazole-carboxamide derivatives as anticancer agents

The present study aimed to design and synthesize a series of phenyl-isoxazole-carboxamide derivatives and investigate their antitumor and antioxidant activities. The in vitro cytotoxic evaluation was conducted using the MTS assay against four cancer cell lines: hepatocellular carcinoma (Hep3B and HepG2), cervical adenocarcinoma (HeLa), breast carcinoma (MCF-7), in addition to the normal cell line (Hek293T). Besides, the antioxidant activity was evaluated using a 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. All obtained compounds were found to have potent to moderate activities against Hep3B and MCF-7 cancer cells lines, except compound 2e. It was found that compound 2a has potent activity against HeLa and Hep3B cancer cell lines with IC50 values of 0.91 and 8.02 mu M, respectively. The IC50 dose range of the tested compounds against Hep3B was 5.96-28.62 mu M, except for 2e, compared with doxorubicin, which has an IC50 value of 2.23 mu M. Also, the IC50 value range of the compounds against Hek293T was 112.78-266.66 mu M, compared with doxorubicin, which has an IC50 dose of 0.581 mu M. The antioxidant activity of the synthesized compounds was weak, and compound 2d showed moderate activity against the DPPH enzyme with an IC50 value of 138.50 mu M in comparison with Trolox, which has an IC50 dose of 37.23 mu M.

Automated summary

The study involved the design and synthesis of a series of phenyl-isoxazole-carboxamide derivatives to assess their antitumor and antioxidant activities. The compounds showed potent to moderate activities against certain cancer cell lines, with compound 2a demonstrating strong activity against HeLa and Hep3B cancer cells. However, the antioxidant activity of the synthesized compounds was found to be weak.