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 µM, respectively. The IC₅₀ dose range of the tested compounds against Hep3B was 5.96–28.62 µM, except for 2e, compared with doxorubicin, which has an IC₅₀ value of 2.23 µM. Also, the IC₅₀ value range of the compounds against Hek293T was 112.78–266.66 µM, compared with doxorubicin, which has an IC₅₀ dose of 0.581 µM. 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 µM in comparison with Trolox, which has an IC₅₀ dose of 37.23 µM.

Title

Heterocyclic Communications

Publisher

Walter de Gruyter GmbH

Publisher Country

Germany

Indexing

Thomson Reuters

Impact Factor

1.15

Publication Type

Prtinted only

Volume

27

Year

2021

Pages

133-141