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The current study aimed to design and synthesize a novel series of fluorophenyl-isoxazole-carboxamide derivatives and evaluate their antiproliferative activities. Anticancer activities of the novel compounds were evaluated by MTS assay against four cancer cell lines, including liver (Hep3B, HepG2), cervical (HeLa), and breast (MCF-7), and  α -fetoprotein tumor marker, cell cycle analysis, and annexin V tests. Chemo-informatics analysis showed that all synthesized derivatives  2a–2f  obeyed Lipinski’s rule. Compound  2f  was the most potent compound against Hep3B and Hep-G2 cancer cell lines with IC 50  values of 5.76 and 34.64 µg/mL, respectively. Moreover, compounds  2a–2c  and  2e  showed potent inhibitory activity against Hep3B with an IC 50  value range of 7.66–11.60 µg/mL. Hep3B secretions of  α -fetoprotein ( α -FP) results showed that compound  2f  reduced the secretion of Hep3B to 168.33 ng/mL and compound  2d  reduced the secretion to value approximately 598.33 ng/mL, in comparison with untreated cells’ value of 1116.67 ng/mL. Furthermore, cell cycle analysis showed that the  2f  compound induced arrest in the G2-M phase in 6.73% of the total cells and that was lower than the activity of the positive control doxorubicin (7.4%). Moreover,  2b  and  2f  compounds reduced the necrosis rate of Hep3B to 4-folds and shifted the cells to apoptosis.

Synthesis, chemo-informatics, and anticancer evaluation of fluorophenyl-isoxazole derivatives