دورية أكاديمية
Synthesis, chemo-informatics, and anticancer evaluation of fluorophenyl-isoxazole derivatives
| العنوان: | Synthesis, chemo-informatics, and anticancer evaluation of fluorophenyl-isoxazole derivatives |
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| المؤلفون: | Hawash Mohammed, Jaradat Nidal, Abualhasan Murad, Amer Johnny, Levent Serkan, Issa Shahd, Ibrahim Sameeha, Ayaseh Aseel, Shtayeh Tahrir, Mousa Ahmed |
| المصدر: | Open Chemistry, Vol 19, Iss 1, Pp 855-863 (2021) |
| بيانات النشر: | De Gruyter, 2021. |
| سنة النشر: | 2021 |
| المجموعة: | LCC:Chemistry |
| مصطلحات موضوعية: | isoxazole, anticancer, hep3b, doxorubicin, Chemistry, QD1-999 |
| الوصف: | 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 IC50 values of 5.76 and 34.64 µg/mL, respectively. Moreover, compounds 2a–2c and 2e showed potent inhibitory activity against Hep3B with an IC50 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. |
| نوع الوثيقة: | article |
| وصف الملف: | electronic resource |
| اللغة: | English |
| تدمد: | 2391-5420 2021-0078 |
| Relation: | https://doaj.org/toc/2391-5420 |
| DOI: | 10.1515/chem-2021-0078 |
| URL الوصول: | https://doaj.org/article/1e00ebae391745c98a4cd8fbdb12fd31 |
| رقم الأكسشن: | edsdoj.1e00ebae391745c98a4cd8fbdb12fd31 |
| قاعدة البيانات: | Directory of Open Access Journals |
Full Text Finder | تدمد: | 23915420 20210078 |
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| DOI: | 10.1515/chem-2021-0078 |