An article Rational Design and Synthesis of Diverse Pyrimidine Molecules Bearing Sulfonamide Moiety as Novel ERK Inhibitors WOS:000502786800074 published article about CARBONIC-ANHYDRASE INHIBITORS; BIOLOGICAL EVALUATION; ANTIPROLIFERATIVE ACTIVITY; ANTIMICROBIAL ACTIVITIES; DERIVATIVES; PYRAZOLE; ANTICANCER; DOCKING; COMPLEXES; RELEASE in [Halawa, Ahmed H.; Elgammal, Walid E.; Hassan, Saber M.; Hassan, Ahmed H.; El-Agrody, Ahmed M.] Al Azhar Univ, Fac Sci, Chem Dept, Cairo 11284, Egypt; [Eskandrani, Areej A.; Okasha, Rawda M.] Taibah Univ, Fac Sci, Chem Dept, Medina 30002, Saudi Arabia; [Hassan, Ahmed H.] Jazan Univ, Fac Sci, Chem Dept, Jazan 45142, Saudi Arabia; [Ebrahim, Hassan Y.] Helwan Univ, Fac Pharm, Pharmacognosy Dept, Cairo 11795, Egypt; [Mehany, Ahmed B. M.] Al Azhar Univ, Fac Sci, Zool Dept, Cairo 11284, Egypt in 2019.0, Cited 65.0. The Name is 1H-1,2,4-Triazol-5-amine. Through research, I have a further understanding and discovery of 61-82-5. Recommanded Product: 1H-1,2,4-Triazol-5-amine
Protein kinases orchestrate diverse cellular functions; however, their dysregulation is linked to metabolic dysfunctions, associated with many diseases, including cancer. Mitogen-Activated Protein (MAP) kinase is a notoriously oncogenic signaling pathway in human malignancies, where the extracellular signal-regulated kinases (ERK1/2) are focal serine/threonine kinases in the MAP kinase module with numerous cytosolic and nuclear mitogenic effector proteins. Subsequently, hampering the ERK kinase activity by small molecule inhibitors is a robust strategy to control the malignancies with aberrant MAP kinase signaling cascades. Consequently, new heterocyclic compounds, containing a sulfonamide moiety, were rationally designed, aided by the molecular docking of the starting reactant 1-(4-((4-methylpiperidin-1-yl)sulfonyl)phenyl)ethan-1-one (3) at the ATP binding pocket of the ERK kinase domain, which was relying on the molecular extension tactic. The identities of the synthesized compounds (4-33) were proven by their spectral data and elemental analysis. The target compounds exhibited pronounced anti-proliferative activities against the MCF-7, HepG-2, and HCT-116 cancerous cell lines with potencies reaching a 2.96 mu M for the most active compound (22). Moreover, compounds 5, 9, 10b, 22, and 28 displayed a significant G2/M phase arrest and induction of the apoptosis, which was confirmed by the cell cycle analysis and the flow cytometry. Thus, the molecular extension of a small fragment bounded at the ERK kinase domain is a valid tactic for the rational synthesis of the ERK inhibitors to control various human malignancies.
Recommanded Product: 1H-1,2,4-Triazol-5-amine. About 1H-1,2,4-Triazol-5-amine, If you have any questions, you can contact Halawa, AH; Eskandrani, AA; Elgammal, WE; Hassan, SM; Hassan, AH; Ebrahim, HY; Mehany, ABM; El-Agrody, AM; Okasha, RM or concate me.
Reference:
Article; Safari, Niloufar; Shirini, Farhad; Tajik, Hassan; Journal of Molecular Structure; vol. 1201; (2020);,
1,2,3-Triazole – Wikipedia,
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