التفاصيل البيبلوغرافية
| العنوان: |
New 1,2,3-triazole/1,2,4-triazole hybrids linked to oxime moiety as nitric oxide donor selective COX-2, aromatase, B-RAFV600E and EGFR inhibitors celecoxib analogs: design, synthesis, anti-inflammatory/anti-proliferative activities, apoptosis and molecular modeling study |
| المؤلفون: |
Fadaly, Wael A. A., Nemr, Mohamed T. M., Zidan, Taha H., Mohamed, Fatma E. A., Abdelhakeem, Marwa M., Abu Jayab, Nour N., Omar, Hany A., Abdellatif, Khaled R. A. |
| المصدر: |
Journal of Enzyme Inhibition & Medicinal Chemistry; Dec2023, Vol. 38 Issue 1, p1-23, 23p |
| مصطلحات موضوعية: |
AROMATASE, MOIETIES (Chemistry), EPIDERMAL growth factor receptors, CYCLOOXYGENASE 2, CELECOXIB, NITRIC oxide, OXIME derivatives |
| مستخلص: |
A new series of bis-triazole 19a-l was synthesised for the purpose of being hybrid molecules with both anti-inflammatory and anti-cancer activities and assessed for cell cycle arrest, NO release. Compounds 19c, 19f, 19h, 19 l exhibited COX-2 selectivity indexes in the range of 18.48 to 49.38 compared to celecoxib S.I. = 21.10), inhibit MCF-7 with IC50 = 9–16 μM compared to tamoxifen (IC50 = 27.9 μM). and showed good inhibitory activity against HEP-3B with IC50 = 4.5–14 μM compared to sorafenib (IC50 = 3.5 μM) (HEP-3B). Moreover, derivatives 19e, 19j, 19k, 19 l inhibit HCT-116 with IC50 = 5.3–13.7 μM compared to 5-FU with IC50 = 4.8 μM (HCT-116). Compounds 19c, 19f, 19h, 19 l showed excellent inhibitory activity against A549 with IC50 = 3–4.5 μM compared to 5-FU with IC50 = 6 μM (A549). Compounds 19c, 19f, 19h, 19 l inhibit aromatase (IC50 of 22.40, 23.20, 22.70, 30.30 μM), EGFR (IC50 of 0.112, 0.205, 0.169 and 0.066 μM) and B-RAFV600E (IC50 of 0.09, 0.06, 0.07 and 0.05 μM). [ABSTRACT FROM AUTHOR] |
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| قاعدة البيانات: |
Complementary Index |
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