Cancer now is one of the leading causes of mortality in the world. There has been a lot of effort to discover new anticarcinogenic
agents that allow treatment with fewer side effects. A series of isoxazole-carboxamide derivatives (2a–2g) were synthesised and
evaluated for their cytotoxic activity against breast (MCF-7), cervical (HeLa), and liver (Hep3B) cancer cell lines and their
antioxidant activity in the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. The results showed that 2d and 2e were the most active
compounds against Hep3B cells, with a half-maximal inhibitory concentration (IC50) of around 23 μg/ml; 2d showed the highest
activity against HeLa cells, with an IC50 15.48 μg/ml. However, 2a had the lowest IC50 (39.80 μg/ml) against MCF-7 cells. By
contrast, compound 2g was inactive against all cancer cell lines, with IC50 values >400 μg/ml. Both 2d and 2e reduced Hep3B
secretion of alpha-fetoprotein (to 1829:33 ± 65:91 ng/ml and 1758:66 ± 54:04 ng/ml, respectively). Furthermore, in cell cycle
analysis, 2d and 2e induced a delay in the G2/M phase of 18.07%, which is similar to the doxorubicin positive control.
Moreover, 2d and 2e reduced the necrosis rate of Hep3B threefold and instead shifted the cells to apoptosis. Our results indicate
that 2d and 2e have potent and promising anticancer activity. However, compound 2a was the most active as antioxidant agent
(IC50 = 7:8 ± 1:21 μg/ml) compared with Trolox as a positive control (IC50 2.75 μg/ml).

Title

BioMed Research International

Publisher

Hindawi

Publisher Country

United Kingdom

Indexing

Thomson Reuters

Impact Factor

2.276

Publication Type

Both (Printed and Online)

Volume

2021

Year

2021

Pages

9